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Carlo Melchiorre
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43
Minarini, Anna
38
Rosini, Michela
38
Bolognesi, Maria Laura
34
Tumiatti, Vincenzo
29
Giardinà, Dario
23
Marucci, Gabriella
22
Andrisano, Vincenza
19
Quaglia, Wilma
18
Angeli, Piero
18
Budriesi, Roberta
18
Brasili, Livio
17
Chiarini, Alberto
17
Bartolini, Manuela
15
Cavalli, Andrea
13
Leonardi, Amedeo
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All Publications
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2009: Zini Maddalena; Passariello Catherine L; Gottardi Davide; Cetrullo Silvia; Flamigni Flavio; Pignatti Carla; Minarini Anna; Tumiatti Vincenzo; Milelli Andrea; Melchiorre Carlo; Stefanelli Claudio
Cytotoxicity of methoctramine and methoctramine-related polyamines.
Chemico-biological interactions 2009;181(3):409-16.
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2009: Mancini Francesca; Bolognesi Maria Laura; Melchiorre Carlo; Andrisano Vincenza
Investigation of the photostability properties of memoquin, a quinone derivative for the treatment of Alzheimer's disease.
Journal of pharmaceutical and biomedical analysis 2009;50(2):164-70.
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2009: Giardinà Dario; Martarelli Daniele; Sagratini Gianni; Angeli Piero; Ballinari Dario; Gulini Ugo; Melchiorre Carlo; Poggesi Elena; Pompei Pierluigi
Doxazosin-related alpha1-adrenoceptor antagonists with prostate antitumor activity.
Journal of medicinal chemistry 2009;52(15):4951-4.
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2009: Bolognesi Maria Laura; Bartolini Manuela; Rosini Michela; Andrisano Vincenza; Melchiorre Carlo
Structure-activity relationships of memoquin: Influence of the chain chirality in the multi-target mechanism of action.
Bioorganic & medicinal chemistry letters 2009;19(15):4312-5.
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2009: Bolognesi Maria L; Matera Riccardo; Minarini Anna; Rosini Michela; Melchiorre Carlo
Alzheimer's disease: new approaches to drug discovery.
Current opinion in chemical biology 2009;13(3):303-8.
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2009: Bolognesi Maria Laura; Cavalli Andrea; Melchiorre Carlo
Memoquin: a multi-target-directed ligand as an innovative therapeutic opportunity for Alzheimer's disease.
Neurotherapeutics : the journal of the American Society for Experimental NeuroTherapeutics 2009;6(1):152-62.
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2009: Bolognesi M L; Rosini M; Andrisano V; Bartolini M; Minarini A; Tumiatti V; Melchiorre C
MTDL design strategy in the context of Alzheimer's disease: from lipocrine to memoquin and beyond.
Current pharmaceutical design 2009;15(6):601-13.
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2008: Tumiatti Vincenzo; Milelli Andrea; Minarini Anna; Rosini Michela; Bolognesi Maria Laura; Micco Marialuisa; Andrisano Vincenza; Bartolini Manuela; Mancini Francesca; Recanatini Maurizio; Cavalli Andrea; Melchiorre Carlo
Structure-activity relationships of acetylcholinesterase noncovalent inhibitors based on a polyamine backbone. 4. Further investigation on the inner spacer.
Journal of medicinal chemistry 2008;51(22):7308-12.
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2008: Bolognesi Maria Laura; Minarini Anna; Rosini Michela; Tumiatti Vincenzo; Melchiorre Carlo
From dual binding site acetylcholinesterase inhibitors to multi-target-directed ligands (MTDLs): a step forward in the treatment of Alzheimer's disease.
Mini reviews in medicinal chemistry 2008;8(10):960-7.
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2008: Bolognesi Maria Laura; Calonghi Natalia; Mangano Chiara; Masotti Lanfranco; Melchiorre Carlo
Parallel synthesis and cytotoxicity evaluation of a polyamine-quinone conjugates library.
Journal of medicinal chemistry 2008;51(17):5463-7.
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2008: Rosini Michela; Simoni Elena; Bartolini Manuela; Cavalli Andrea; Ceccarini Luisa; Pascu Nicoleta; McClymont David W; Tarozzi Andrea; Bolognesi Maria L; Minarini Anna; Tumiatti Vincenzo; Andrisano Vincenza; Mellor Ian R; Melchiorre Carlo
Inhibition of acetylcholinesterase, beta-amyloid aggregation, and NMDA receptors in Alzheimer's disease: a promising direction for the multi-target-directed ligands gold rush.
Journal of medicinal chemistry 2008;51(15):4381-4.
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2008: Minarini Anna; Marucci Gabriella; Bellucci Cristina; Giorgi Gianluca; Tumiatti Vincenzo; Bolognesi Maria Laura; Matera Riccardo; Rosini Michela; Melchiorre Carlo
Design, synthesis, and biological evaluation of pirenzepine analogs bearing a 1,2-cyclohexanediamine and perhydroquinoxaline units in exchange for the piperazine ring as antimuscarinics.
Bioorganic & medicinal chemistry 2008;16(15):7311-20.
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2008: Cavalli Andrea; Bolognesi Maria Laura; Minarini Anna; Rosini Michela; Tumiatti Vincenzo; Recanatini Maurizio; Melchiorre Carlo
Multi-target-directed ligands to combat neurodegenerative diseases.
Journal of medicinal chemistry 2008;51(3):347-72.
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2007: Bolognesi Maria Laura; Cavalli Andrea; Valgimigli Luca; Bartolini Manuela; Rosini Michela; Andrisano Vincenza; Recanatini Maurizio; Melchiorre Carlo
Multi-target-directed drug design strategy: from a dual binding site acetylcholinesterase inhibitor to a trifunctional compound against Alzheimer's disease.
Journal of medicinal chemistry 2007;50(26):6446-9.
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2007: Mancini Francesca; Bolognesi Maria L; Melchiorre Carlo; Cavalli Andrea; Andrisano Vincenza
Monolithic stationary phase coupled with coulometric detection: development of an ion-pair HPLC method for the analysis of quinone-bearing compounds.
Journal of separation science 2007;30(17):2935-42.
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2007: Bartolini Manuela; Bertucci Carlo; Bolognesi Maria Laura; Cavalli Andrea; Melchiorre Carlo; Andrisano Vincenza
Insight into the kinetic of amyloid beta (1-42) peptide self-aggregation: elucidation of inhibitors' mechanism of action.
Chembiochem : a European journal of chemical biology 2007;8(17):2152-61.
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2007: Bolognesi Maria Laura; Banzi Rita; Bartolini Manuela; Cavalli Andrea; Tarozzi Andrea; Andrisano Vincenza; Minarini Anna; Rosini Michela; Tumiatti Vincenzo; Bergamini Christian; Fato Romana; Lenaz Giorgio; Hrelia Patrizia; Cattaneo Antonino; Recanatini Maurizio; Melchiorre Carlo
Novel class of quinone-bearing polyamines as multi-target-directed ligands to combat Alzheimer's disease.
Journal of medicinal chemistry 2007;50(20):4882-97.
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2007: Tumiatti Vincenzo; Minarini Anna; Milelli Andrea; Rosini Michela; Buccioni Michela; Marucci Gabriella; Ghelardini Carla; Bellucci Cristina; Melchiorre Carlo
Structure-activity relationships of methoctramine-related polyamines as muscarinic antagonist: effect of replacing the inner polymethylene chain with cyclic moieties.
Bioorganic & medicinal chemistry 2007;15(6):2312-21.
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2007: Sagratini Gianni; Angeli Piero; Buccioni Michela; Gulini Ugo; Marucci Gabriella; Melchiorre Carlo; Leonardi Amedeo; Poggesi Elena; Giardinà Dario
Synthesis and alpha(1)-adrenoceptor antagonist activity of derivatives and isosters of the furan portion of (+)-cyclazosin.
Bioorganic & medicinal chemistry 2007;15(6):2334-45.
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2007: Calonghi N; Pagnotta E; Parolin C; Mangano C; Bolognesi M L; Melchiorre C; Masotti L
A new EGFR inhibitor induces apoptosis in colon cancer cells.
Biochemical and biophysical research communications 2007;354(2):409-13.
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2007: Cavalli Andrea; Bolognesi Maria Laura; Capsoni Simona; Andrisano Vincenza; Bartolini Manuela; Margotti Elisa; Cattaneo Antonino; Recanatini Maurizio; Melchiorre Carlo
A small molecule targeting the multifactorial nature of Alzheimer's disease.
Angewandte Chemie (International ed. in English) 2007;46(20):3689-92.
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2007: Rosini Michela; Bolognesi Maria L; Giardinà Dario; Minarini Anna; Tumiatti Vincenzo; Melchiorre Carlo
Recent advances in alpha1-adrenoreceptor antagonists as pharmacological tools and therapeutic agents.
Current topics in medicinal chemistry 2007;7(2):147-62.
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2006: Rosini Michela; Mancini Francesca; Tarozzi Andrea; Colizzi Francesco; Andrisano Vincenza; Bolognesi Maria L; Hrelia Patrizia; Melchiorre Carlo
Design, synthesis, and biological evaluation of substituted 2,3-dihydro-1H-cyclopenta[b]quinolin-9-ylamine related compounds as fructose-1,6-bisphosphatase inhibitors.
Bioorganic & medicinal chemistry 2006;14(23):7846-53.
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2006: Antonello Alessandra; Tarozzi Andrea; Morroni Fabiana; Cavalli Andrea; Rosini Michela; Hrelia Patrizia; Bolognesi Maria Laura; Melchiorre Carlo
Multitarget-directed drug design strategy: a novel molecule designed to block epidermal growth factor receptor (EGFR) and to exert proapoptotic effects.
Journal of medicinal chemistry 2006;49(23):6642-5.
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2006: Bolognesi Maria L; Minarini Anna; Tumiatti Vincenzo; Melchiorre Carlo
Lipoic acid, a lead structure for multi-target-directed drugs for neurodegeneration.
Mini reviews in medicinal chemistry 2006;6(11):1269-74.
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2005: Marucci Gabriella; Angeli Piero; Buccioni Michela; Gulini Ugo; Melchiorre Carlo; Sagratini Gianni; Testa Rodolfo; Giardinà Dario
(+)-Cyclazosin, a selective alpha1B-adrenoceptor antagonist: functional evaluation in rat and rabbit tissues.
European journal of pharmacology 2005;522(1-3):100-7.
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2005: Bolognesi Maria Laura; Andrisano Vincenza; Bartolini Manuela; Cavalli Andrea; Minarini Anna; Recanatini Maurizio; Rosini Michela; Tumiatti Vincenzo; Melchiorre Carlo
Heterocyclic inhibitors of AChE acylation and peripheral sites.
Farmaco (Società chimica italiana : 1989) 2005;60(6-7):465-73.
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2005: Rosini Michela; Andrisano Vincenza; Bartolini Manuela; Bolognesi Maria L; Hrelia Patrizia; Minarini Anna; Tarozzi Andrea; Melchiorre Carlo
Rational approach to discover multipotent anti-Alzheimer drugs.
Journal of medicinal chemistry 2005;48(2):360-3.
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2005: Antonello Alessandra; Hrelia Patrizia; Leonardi Amedeo; Marucci Gabriella; Rosini Michela; Tarozzi Andrea; Tumiatti Vincenzo; Melchiorre Carlo
Design, synthesis, and biological evaluation of prazosin-related derivatives as multipotent compounds.
Journal of medicinal chemistry 2005;48(1):28-31.
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2005: Bolognesi Maria Laura; Andrisano Vincenza; Bartolini Manuela; Banzi Rita; Melchiorre Carlo
Propidium-based polyamine ligands as potent inhibitors of acetylcholinesterase and acetylcholinesterase-induced amyloid-beta aggregation.
Journal of medicinal chemistry 2005;48(1):24-7.
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2004: Giardinà Dario; Sagratini Gianni; Grelli Massimo; Gulini Ugo; Melchiorre Carlo; Antolini Luciano
Absolute configuration of the alpha (1B)-adrenoceptor antagonist (+)-cyclazosin.
Farmaco (Società chimica italiana : 1989) 2004;59(12):965-9.
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2004: Tumiatti Vincenzo; Andrisano Vincenza; Banzi Rita; Bartolini Manuela; Minarini Anna; Rosini Michela; Melchiorre Carlo
Structure-activity relationships of acetylcholinesterase noncovalent inhibitors based on a polyamine backbone. 3. Effect of replacing the inner polymethylene chain with cyclic moieties.
Journal of medicinal chemistry 2004;47(26):6490-8.
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2004: Mellor Ian R; Ogilvie Jane; Pluteanu Florentina; Clothier Richard H; Parker Terence L; Rosini Michela; Minarini Anna; Tumiatti Vincenzo; Melchiorre Carlo
Methoctramine analogues inhibit responses to capsaicin and protons in rat dorsal root ganglion neurons.
European journal of pharmacology 2004;505(1-3):37-50.
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2004: Bolognesi Maria Laura; Bartolini Manuela; Cavalli Andrea; Andrisano Vincenza; Rosini Michela; Minarini Anna; Melchiorre Carlo
Design, synthesis, and biological evaluation of conformationally restricted rivastigmine analogues.
Journal of medicinal chemistry 2004;47(24):5945-52.
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2003: Rosini Michela; Antonello Alessandra; Cavalli Andrea; Bolognesi Maria L; Minarini Anna; Marucci Gabriella; Poggesi Elena; Leonardi Amedeo; Melchiorre Carlo
Prazosin-related compounds. Effect of transforming the piperazinylquinazoline moiety into an aminomethyltetrahydroacridine system on the affinity for alpha1-adrenoreceptors.
Journal of medicinal chemistry 2003;46(23):4895-903.
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2003: Bolognesi Maria Laura; Cavalli Andrea; Andrisano Vincenza; Bartolini Manuela; Banzi Rita; Antonello Alessandra; Rosini Michela; Melchiorre Carlo
Design, synthesis and biological evaluation of ambenonium derivatives as AChE inhibitors.
Farmaco (Società chimica italiana : 1989) 2003;58(9):917-28.
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2003: Giardinà Dario; Polimanti O; Sagratini G; Angeli P; Gulini U; Marucci G; Melchiorre C; Poggesi E; Leonardi A
Searching for cyclazosin analogues as alpha(1B)-adrenoceptor antagonists.
Farmaco (Società chimica italiana : 1989) 2003;58(7):477-87.
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2003: Tumiatti Vincenzo; Rosini Michela; Bartolini Manuela; Cavalli Andrea; Marucci Gabriella; Andrisano Vincenza; Angeli Piero; Banzi Rita; Minarini Anna; Recanatini Maurizio; Melchiorre Carlo
Structure-activity relationships of acetylcholinesterase noncovalent inhibitors based on a polyamine backbone. 2. Role of the substituents on the phenyl ring and nitrogen atoms of caproctamine.
Journal of medicinal chemistry 2003;46(6):954-66.
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2003: Melchiorre Carlo; Antonello Alessandra; Banzi Rita; Bolognesi Maria Laura; Minarini Anna; Rosini Michela; Tumiatti Vincenzo
Polymethylene tetraamine backbone as template for the development of biologically active polyamines.
Medicinal research reviews 2003;23(2):200-33.
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2002: Bolognesi Maria L; Bixel M Gabriele; Marucci Gabriella; Bartolini Manuela; Krauss Michael; Angeli Piero; Antonello Alessandra; Rosini Michela; Tumiatti Vincenzo; Hucho Ferdinand; Melchiorre Carlo
Structure-activity relationships of methoctramine-related polyamines as muscular nicotinic receptor noncompetitive antagonists. 3. Effect of inserting the tetraamine backbone into a macrocyclic structure.
Journal of medicinal chemistry 2002;45(15):3286-95.
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2002: Giardinà Dario; Crucianelli Mauro; Angeli Piero; Buccioni Michela; Gulini Ugo; Marucci Gabriella; Sagratini Gianni; Melchiorre Carlo
Structure--activity relationships among novel phenoxybenzamine-related beta-chloroethylamines.
Bioorganic & medicinal chemistry 2002;10(5):1291-303.
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2002: Rosini Michela; Bixel M Gabriele; Marucci Gabriella; Budriesi Roberta; Krauss Michael; Bolognesi Maria L; Minarini Anna; Tumiatti Vincenzo; Hucho Ferdinand; Melchiorre Carlo
Structure-activity relationships of methoctramine-related polyamines as muscular nicotinic receptor noncompetitive antagonists. 2. Role of polymethylene chain lengths separating amine functions and of substituents on the terminal nitrogen atoms.
Journal of medicinal chemistry 2002;45(9):1860-78.
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2002: Quaglia Wilma; Pigini Maria; Piergentili Alessandro; Giannella Mario; Gentili Francesco; Marucci Gabriella; Carrieri Antonio; Carotti Angelo; Poggesi Elena; Leonardi Amedeo; Melchiorre Carlo
Structure-activity relationships in 1,4-benzodioxan-related compounds. 7. Selectivity of 4-phenylchroman analogues for alpha(1)-adrenoreceptor subtypes.
Journal of medicinal chemistry 2002;45(8):1633-43.
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2001: Melchiorre C; Bolognesi M L; Budriesi R; Ghelardini C; Chiarini A; Minarini A; Rosini M; Tumiatti V; Wade E J
Design, synthesis, and biological activity of methoctramine-related polyamines as putative G(i) protein activators.
Journal of medicinal chemistry 2001;44(24):4035-8.
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2001: Budriesi R; Cacciaguerra S; Toro R D; Bolognesi M L; Chiarini A; Minarini A; Rosini M; Spampinato S; Tumiatti V; Melchiorre C
Analysis of the muscarinic receptor subtype mediating inhibition of the neurogenic contractions in rabbit isolated vas deferens by a series of polymethylene tetra-amines.
British journal of pharmacology 2001;132(5):1009-16.
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2001: Bixel M G; Weise C; Bolognesi M L; Rosini M; Brierly M J; Mellor I R; Usherwood P N; Melchiorre C; Hucho F
Location of the polyamine binding site in the vestibule of the nicotinic acetylcholine receptor ion channel.
The Journal of biological chemistry 2001;276(9):6151-60.
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2001: Bolognesi M L; Marucci G; Angeli P; Buccioni M; Minarini A; Rosini M; Tumiatti V; Melchiorre C
Analogues of prazosin that bear a benextramine-related polyamine backbone exhibit different antagonism toward alpha1-adrenoreceptor subtypes.
Journal of medicinal chemistry 2001;44(3):362-71.
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2001: Bixel M G; Krauss M; Weise C; Bolognesi M L; Rosini M; Usherwood P N; Melchiorre C; Hucho F
Binding of polyamine-containing toxins in the vestibule of the nicotinic acetylcholine receptor ion channel.
Farmaco (Società chimica italiana : 1989) 2001;56(1-2):133-5.
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2001: Li Y; Popaj K; Lochner M; Geneste H; Budriesi R; Chiarini A; Melchiorre C; Hesse M
Analogues of polyamine alkaloids and their synthetic advantages.
Farmaco (Società chimica italiana : 1989) 2001;56(1-2):127-31.
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2001: Bolognesi M L; Andrisano V; Bartolini M; Minarini A; Rosini M; Tumiatti V; Melchiorre C
Hexahydrochromeno[4,3-b]pyrrole derivatives as acetylcholinesterase inhibitors.
Journal of medicinal chemistry 2001;44(1):105-9.
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2000: Tumiatti V; Angeli P; Andrisano V; Bolognesi M L; Cavalli A; Marucci G; Minarini A; Recanatini M; Rosini M; Melchiorre C
[4-[[N-(3-chlorophenyl)carbamoyl]oxy]-2-butynyl]-trimethylammonium (McN-A-343)-related compounds. Effect of the butynyl chain inclusion into an aromatic unit on the potency for muscarinic receptors.
Bioorganic & medicinal chemistry 2000;8(4):681-9.
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2000: Melchiorre C; Angeli P; Bolognesi M L; Chiarini A; Giardinà D; Gulini U; Leonardi A; Marucci G; Minarini A; Pigini M; Quaglia W; Rosini M; Tumiatti V
Alpha 1-adrenoreceptor antagonists bearing a quinazoline or a benzodioxane moiety.
Pharmaceutica acta Helvetiae 2000;74(2-3):181-90.
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2000: D'Agostino G; Bolognesi M L; Lucchelli A; Vicini D; Balestra B; Spelta V; Melchiorre C; Tonini M
Prejunctional muscarinic inhibitory control of acetylcholine release in the human isolated detrusor: involvement of the M4 receptor subtype.
British journal of pharmacology 2000;129(3):493-500.
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2000: Bixel M G; Krauss M; Liu Y; Bolognesi M L; Rosini M; Mellor I S; Usherwood P N; Melchiorre C; Nakanishi K; Hucho F
Structure-activity relationship and site of binding of polyamine derivatives at the nicotinic acetylcholine receptor.
European journal of biochemistry / FEBS 2000;267(1):110-20.
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1999: Rosini M; Budriesi R; Bixel M G; Bolognesi M L; Chiarini A; Hucho F; Krogsgaard-Larsen P; Mellor I R; Minarini A; Tumiatti V; Usherwood P N; Melchiorre C
Design, synthesis, and biological evaluation of symmetrically and unsymmetrically substituted methoctramine-related polyamines as muscular nicotinic receptor noncompetitive antagonists.
Journal of medicinal chemistry 1999;42(25):5212-23.
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1999: Bolognesi M L; Budriesi R; Cavalli A; Chiarini A; Gotti R; Leonardi A; Minarini A; Poggesi E; Recanatini M; Rosini M; Tumiatti V; Melchiorre C
WB 4101-related compounds. 2. Role of the ethylene chain separating amine and phenoxy units on the affinity for alpha(1)-adrenoreceptor subtypes and 5-HT(1A) receptors.
Journal of medicinal chemistry 1999;42(20):4214-24.
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1999: Quaglia W; Pigini M; Piergentili A; Giannella M; Marucci G; Poggesi E; Leonardi A; Melchiorre C
Structure-activity relationships in 1,4-benzodioxan-related compounds. 6. Role of the dioxane unit on selectivity for alpha(1)-adrenoreceptor subtypes.
Journal of medicinal chemistry 1999;42(15):2961-8.
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1998: Bolognesi M L; Budriesi R; Chiarini A; Poggesi E; Leonardi A; Melchiorre C
Design, synthesis, and biological activity of prazosin-related antagonists. Role of the piperazine and furan units of prazosin on the selectivity for alpha1-adrenoreceptor subtypes.
Journal of medicinal chemistry 1998;41(24):4844-53.
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1998: Melchiorre C; Andrisano V; Bolognesi M L; Budriesi R; Cavalli A; Cavrini V; Rosini M; Tumiatti V; Recanatini M
Acetylcholinesterase noncovalent inhibitors based on a polyamine backbone for potential use against Alzheimer's disease.
Journal of medicinal chemistry 1998;41(22):4186-9.
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1998: Bolognesi M L; Minarini A; Budriesi R; Cacciaguerra S; Chiarini A; Spampinato S; Tumiatti V; Melchiorre C
Universal template approach to drug design: polyamines as selective muscarinic receptor antagonists.
Journal of medicinal chemistry 1998;41(21):4150-60.
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1998: Barbier P; Colelli A; Bolognesi M L; Minarini A; Tumiatti V; Corsini G U; Melchiorre C; Maggio R
Antagonist binding profile of the split chimeric muscarinic m2-trunc/m3-tail receptor.
European journal of pharmacology 1998;355(2-3):267-74.
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1998: Minarini A; Budriesi R; Chiarini A; Leonardi A; Melchiorre C
Search for alpha 1-adrenoceptor subtypes selective antagonists: design, synthesis and biological activity of cystazosin, an alpha 1D-adrenoceptor antagonist.
Bioorganic & medicinal chemistry letters 1998;8(11):1353-8.
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1998: Quaglia W; Giannella M; Piergentili A; Pigini M; Brasili L; Di Toro R; Rossetti L; Spampinato S; Melchiorre C
1'-Benzyl-3,4-dihydrospiro[2H-1- benzothiopyran-2,4'-piperidine] (spipethiane), a potent and highly selective sigma1 ligand.
Journal of medicinal chemistry 1998;41(10):1557-60.
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1998: Melchiorre C; Bolognesi M L; Budriesi R; Chiarini A; Giardinà D; Minarini A; Quaglia W; Leonardi A
Search for selective antagonists at alpha 1-adrenoreceptors: neutral or negative antagonism?
Farmaco (Società chimica italiana : 1989) 1998;53(4):278-86.
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1997: Giardinà D; Crucianelli M; Marucci G; Angeli P; Melchiorre C; Antolini L
Synthesis and alpha-adrenoceptor blocking activity of the enantiomers of benzyl-(2-chloroethyl)-[2-(2-methoxyphenoxy)-1-methylethyl]amine hydrochloride.
Bioorganic & medicinal chemistry 1997;5(9):1775-82.
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1996: Giardinà D; Crucianelli M; Marucci G; Melchiorre C; Polidori C; Pompei P; Massi M
Pharmacological evaluation of prazosin- and doxazosin-related compounds with modified piperazine ring.
Arzneimittel-Forschung 1996;46(11):1054-9.
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1996: Giardinà D; Crucianelli M; Romanelli R; Leonardi A; Poggesi E; Melchiorre C
Synthesis and biological profile of the enantiomers of [4-(4-amino-6,7-dimethoxyquinazolin-2-yl)-cis-octahydroquinoxalin- 1-yl]furan-2-ylmethanone (cyclazosin), a potent competitive alpha 1B- adrenoceptor antagonist.
Journal of medicinal chemistry 1996;39(23):4602-7.
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1996: Quaglia W; Pigini M; Tayebati S K; Piergentili A; Giannella M; Leonardi A; Taddei C; Melchiorre C
Synthesis, absolute configuration, and biological profile of the enantiomers of trans-[2-(2,6-dimethoxyphenoxy)ethyl] [(3-p-tolyl-2,3-dihydro-1,4-benzodioxin-2-yl)methyl]amine (mephendioxan), a potent competitive alpha 1A-adrenoreceptor antagonist.
Journal of medicinal chemistry 1996;39(11):2253-8.
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1996: Quaglia W; Giannella M; Marucci G; Piergentili A; Pigini M; Tayebati S K; Melchiorre C
Structure-activity relationships in 1,4-benzodioxan-related compounds. 5. Effects of modification of the side chain on alpha-adrenoreceptor blocking activity.
Farmaco (Società chimica italiana : 1989) 1996;51(1):27-32.
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1995: Giardinà D; Crucianelli M; Melchiorre C; Taddei C; Testa R
Receptor binding profile of cyclazosin, a new alpha 1B-adrenoceptor antagonist.
European journal of pharmacology 1995;287(1):13-6.
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1995: Angeli P; Cantalamessa F; Gulini U; Melchiorre C
Selective blockade of muscarinic M2 receptors in vivo by the new antagonist tripitramine.
Naunyn-Schmiedeberg's archives of pharmacology 1995;352(3):304-7.
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1995: Chiarini A; Budriesi R; Bolognesi M L; Minarini A; Melchiorre C
In vitro characterization of tripitramine, a polymethylene tetraamine displaying high selectivity and affinity for muscarinic M2 receptors.
British journal of pharmacology 1995;114(7):1507-17.
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1995: Recanatini M; Tumiatti V; Budriesi R; Chiarini A; Sabatino P; Bolognesi M L; Melchiorre C
Synthesis, muscarinic blocking activity and molecular modeling studies of 4-DAMP-related compounds.
Bioorganic & medicinal chemistry 1995;3(3):267-77.
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1995: Giardinà D; Crucianelli M; Marucci G; Paparelli F; Melchiorre C
Synthesis and alpha-adrenoreceptor blocking properties of phenoxybenzamine-related (2-chloroethyl)-(2,3-dihydrobenzo[1,4]dioxin- 2-ylmethyl)-(2-phenoxyethyl) amines.
Bioorganic & medicinal chemistry 1995;3(1):85-94.
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1995: Melchiorre C; Minarini A; Budriesi R; Chiarini A; Spampinato S; Tumiatti V
The design of novel methoctramine-related tetraamines as muscarinic receptor subtype selective antagonists.
Life sciences 1995;56(11-12):837-44.
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1994: Melchiorre C; Romualdi P; Bolognesi M L; Donatini A; Ferri S
Binding profile of benextramine at neuropeptide Y receptor subtypes in rat brain areas.
European journal of pharmacology 1994;265(1-2):93-8.
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1994: Minarini A; Bolognesi M L; Budriesi R; Canossa M; Chiarini A; Spampinato S; Melchiorre C
Design, synthesis, and biological activity of methoctramine-related tetraamines bearing an 11-acetyl-5,11-dihydro-6H-pyrido[2,3-b][1,4] benzodiazepin-6-one moiety: structural requirements for optimum occupancy of muscarinic receptor subtypes as revealed by symmetrical and unsymmetrical polyamines.
Journal of medicinal chemistry 1994;37(20):3363-72.
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1994: Maggio R; Barbier P; Bolognesi M L; Minarini A; Tedeschi D; Melchiorre C
Binding profile of the selective muscarinic receptor antagonist tripitramine.
European journal of pharmacology 1994;268(3):459-62.
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1993: Melchiorre C; Bolognesi M L; Chiarini A; Minarini A; Spampinato S
Synthesis and biological activity of some methoctramine-related tetraamines bearing a 11-acetyl-5,11-dihydro-6H-pyrido[2,3-b][1,4]-benzodiazepin-6-one moiety as antimuscarinics: a second generation of highly selective M2 muscarinic receptor antagonists.
Journal of medicinal chemistry 1993;36(23):3734-7.
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1993: Quaglia W; Pigini M; Tayebati S K; Piergentili A; Giannella M; Marucci G; Melchiorre C
Structure-activity relationships in 1,4-benzodioxan-related compounds. 4. Effect of aryl and alkyl substituents at position 3 on alpha-adrenoreceptor blocking activity.
Journal of medicinal chemistry 1993;36(11):1520-8.
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1993: Giardinà D; Gulini U; Massi M; Piloni M G; Pompei P; Rafaiani G; Melchiorre C
Structure-activity relationships in prazosin-related compounds. 2. Role of the piperazine ring on alpha-blocking activity.
Journal of medicinal chemistry 1993;36(6):690-8.
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1992: v Tumiatti; Recanatini M; Minarini A; Melchiorre C; Budriesi R; Bolognesi M L
Affinity and selectivity at M2 and M3 muscarinic receptor subtypes of cyclic and oxygenated analogues of 4-DAMP.
Farmaco (Società chimica italiana : 1989) 1992;47(9):1133-47.
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1992: Andrisano V; Marucci G; Melchiorre C; Tumiatti V
Stereoselectivity at alpha-adrenoreceptor subtypes: observations with the enantiomers of WB 4101 separated through their amides of N-tosyl-(S)-proline.
Chirality 1992;4(1):16-20.
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1991: Minarini A; Budriesi R; Chiarini A; Melchiorre C; Tumiatti V
Further investigation on methoctramine-related tetraamines: effects of terminal N-substitution and of chain length separating the four nitrogens on M2 muscarinic receptor blocking activity.
Farmaco (Società chimica italiana : 1989) 1991;46(10):1167-78.
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1991: Quaglia W; Giardinà D; Marucci G; Melchiorre C; Minarini A; Tumiatti V
Structure-activity relationships among methoctramine-related polymethylene tetraamines. 3. Effect of the four nitrogens on M2 muscarinic blocking activity as revealed by symmetrical and unsymmetrical polyamines.
Farmaco (Società chimica italiana : 1989) 1991;46(3):417-34.
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1990: Giardinà D; Gulini U; Pigini M; Piloni M G; Melchiorre C
Structure-activity relationships in 1,4-benzodioxan-related compounds. 2. Role of the amine function on alpha-adrenoreceptor blocking activity.
Farmaco (Società chimica italiana : 1989) 1990;45(12):1289-98.
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1990: Quaglia W; Pigini M; Giannella M; Melchiorre C
3-Phenyl analogues of 2-[[[2-(2,6-dimethoxyphenoxy)ethyl]amino]-methyl]-1,4-benzodioxan (WB 4101) as highly selective alpha 1-adrenoceptor antagonists.
Journal of medicinal chemistry 1990;33(11):2946-8.
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1990: Chiarini A; Minarini A; Budriesi R; Melchiorre C
Molecular properties of the histamine H2-receptor. Covalent inhibition by tetraamine disulfides.
Farmaco (Società chimica italiana : 1989) 1990;45(9):1001-11.
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1990: Melchiorre C
Polymethylene tetraamines: a novel class of cardioselective M2-antagonists.
Medicinal research reviews 1990;10(3):327-49.
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1989: Melchiorre C; Minarini A; Angeli P; Giardinà D; Gulini U; Quaglia W
Polymethylene tetraamines as muscarinic receptor probes.
Trends in pharmacological sciences 1989;Suppl():55-9.
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1989: Melchiorre C; Quaglia W; Picchio M T; Giardinà D; Brasili L; Angeli P
Structure-activity relationships among methoctramine-related polymethylene tetraamines. Chain-length and substituent effects on M-2 muscarinic receptor blocking activity.
Journal of medicinal chemistry 1989;32(1):79-84.
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1989: Giardinà D; Brasili L; Gregori M; Massi M; Picchio M T; Quaglia W; Melchiorre C
Structure-activity relationships in prazosin-related compounds. Effect of replacing a piperazine ring with an alkanediamine moiety on alpha 1-adrenoreceptor blocking activity.
Journal of medicinal chemistry 1989;32(1):50-5.
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1988: Melchiorre C; Giardinà D; Gulini U; Pigini M; Quaglia W
Benzodioxanes and quinazolines: probes for characterizing alpha-adrenoreceptors.
Il Farmaco; edizione scientifica 1988;43(12 Suppl):1141-52.
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1988: Pigini M; Brasili L; Giannella M; Giardinà D; Gulini U; Quaglia W; Melchiorre C
Structure-activity relationships in 1,4-benzodioxan-related compounds. Investigation on the role of the dehydrodioxane ring on alpha 1-adrenoreceptor blocking activity.
Journal of medicinal chemistry 1988;31(12):2300-4.
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1988: Quaglia W; Brasili L; Cristalli G; Giardinà D; Picchio M T; Melchiorre C
Structure-activity relationships among benextramine-related tetraamine disulfides. Chain length effect on alpha-adrenoreceptor blocking activity.
Journal of medicinal chemistry 1988;31(9):1861-6.
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1988: Melchiorre C; Cassinelli A; Brasili L; Giardinà D; Gulini U; Quaglia W
Alpha-adrenoceptor occupancy by N,N-dimethyl-2-bromo-2-phenethylamine hydrobromide (DMPEA) in rat vas deferens.
European journal of pharmacology 1988;153(2-3):255-61.
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1987: Melchiorre C; Angeli P; Lambrecht G; Mutschler E; Picchio M T; Wess J
Antimuscarinic action of methoctramine, a new cardioselective M-2 muscarinic receptor antagonist, alone and in combination with atropine and gallamine.
European journal of pharmacology 1987;144(2):117-24.
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1987: Melchiorre C; Cassinelli A; Quaglia W
Differential blockade of muscarinic receptor subtypes by polymethylene tetraamines. Novel class of selective antagonists of cardiac M-2 muscarinic receptors.
Journal of medicinal chemistry 1987;30(1):201-4.
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1986: Massi M; Venturi F; Brasili L; Melchiorre C
Hypotensive effect in dogs and rats of intravenous injections of the alpha 1-adrenoreceptor antagonist benoxathian.
Pharmacological research communications 1986;18(9):813-29.
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1986: Brasili L; Cassinelli A; Angeli P; Melchiorre C
Thiol group may be involved in the irreversible blockade of presynaptic alpha 2-adrenoreceptors by pyrextramine and benextramine in the isolated guinea pig ileum.
Life sciences 1986;38(18):1633-40.
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1985: Angeli P; Brasili L; Brancia E; Giardinà D; Quaglia W; Melchiorre C
Structure-activity relationships among benextramine-related tetraamine disulfides at peripheral alpha-adrenoreceptors.
Journal of medicinal chemistry 1985;28(11):1643-7.
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1985: Giardinà D; Bertini R; Brancia E; Brasili L; Melchiorre C
Structure-activity relationships for prazosin and WB 4101 analogues as alpha 1-adrenoreceptor antagonists.
Journal of medicinal chemistry 1985;28(9):1354-7.
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1984: Melchiorre C; Brasili L; Giardinà D; Pigini M; Strappaghetti G
2-[[[2-(2,6-Dimethoxyphenoxy)ethyl]amino]-methyl] -1,4-benzoxathian: a new antagonist with high potency and selectivity toward alpha 1-adrenoreceptors.
Journal of medicinal chemistry 1984;27(12):1535-6.
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1984: Brasili L; Angeli P; Brancia E; Melchiorre C
N,N''-(dithio-2,1-ethanediyl)bis[N'-(pyrrol-2-ylmethyl)-1, 6,- hexanediamine] (pyrextramine), a new irreversible alpha 1-adrenoreceptor blocking agent of the tetramine disulfide class.
European journal of pharmacology 1984;103(1-2):181-4.
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1983: Melchiorre C; Gallucci P
The irreversible alpha-blocker benextramine interacts with two different thiol groups.
Il Farmaco; edizione scientifica 1983;38(12):950-6.
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1982: Melchiorre C; Giardinà D; Gallucci P; Brasili L
Structural requirements for competitive alpha-adrenoceptor occupancy by cyclic and opened analogues of WB 4101.
The Journal of pharmacy and pharmacology 1982;34(10):683-4.
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1982: Belleau B; Benfey B G; Melchiorre C; Montambault M
Inhibition of adrenaline-induced platelet aggregation by the alpha-adrenoceptor blocking drug benextramine.
British journal of pharmacology 1982;76(2):253-7.
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1982: Belleau B; Benfey B G; Melchiorre C
Presynaptic effect of clonidine antagonized by the tetramine disulphide, benextramine.
British journal of pharmacology 1982;75(4):617-21.
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1982: Belleau B; Benfey B G; Benfey T J; Melchiorre C
Inhibition by the tetramine disulphide, benextramine, of cardiac chronotropic histamine H2-receptor-mediated effects.
British journal of pharmacology 1982;75(4):573-8.
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1981: Angeli P; Brasili L; Giardinà D; Melchiorre C
Molecular requirements of the active site of cholinergic receptors XV: Synthesis and biological activity of 2,3-dehydrodeoxamuscarone and 2,3-dehydrodeoxamuscarines.
Journal of pharmaceutical sciences 1981;70(5):489-92.
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1980: Brasili L; Melchiorre C; Belleau B; Benfey B G
Reactivation by cysteamine of vascular alpha adrenoceptors blocked by the tetramine disulfide benextramine and interaction of benextramine with phenoxybenzamine.
Canadian journal of physiology and pharmacology 1980;58(12):1490-3.
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1980: Benfey B G; Belleau B; Brasili L; Giannella M; Melchiorre C
Irreversible alpha adrenoceptor blocking effects and reversible muscarinic blocking and nicotinic blocking effects of tetramine disulfides on the heart.
Canadian journal of physiology and pharmacology 1980;58(12):1477-83.
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1980: Benfey B G; Brasili L; Melchiorre C; Belleau B
Potentiation and inhibition of nicotinic effects on striated muscle by the tetramine disulfide benextramine.
Canadian journal of physiology and pharmacology 1980;58(8):984-8.
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1980: Giannella M; Angeli P; Melchiorre C; Brasili L
Molecular requirements of the active sites of the cholinergic receptors. XII - 3-Methyl-2-oxo-1-dimethylaminomethylcyclopentane methiodide as a new selective agonist for the nicotinic receptor.
Il Farmaco; edizione scientifica 1980;35(4):253-62.
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