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Carlo Melchiorre

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Maria Laura Bolognesi; Anna Minarini; Michela Rosini; Elena Simoni; Vincenzo Tumiatti; Carlo Melchiorre
Multitarget-directed ligands: innovative chemical probes and therapeutic tools against Alzheimer's disease.
Michela Rosini; Elena Simoni; Andrea Tarozzi; Andrea Milelli; Vincenza Andrisano; Manuela Bartolini; Maria Laura Bolognesi; Patrizia Hrelia; Riccardo Matera; Carlo Melchiorre
Exploiting the lipoic acid structure in the search for novel multitarget ligands against Alzheimer's disease.
Maria Laura Bolognesi; Manuela Bartolini; Andrea Tarozzi; Fabiana Morroni; Federica Lizzi; Andrea Milelli; Anna Minarini; Michela Rosini; Patrizia Hrelia; Vincenza Andrisano; Carlo Melchiorre
Multitargeted drugs discovery: balancing anti-amyloid and anticholinesterase capacity in a single chemical entity.

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All Publications

2011: Maria Laura Bolognesi; Anna Minarini; Michela Rosini; Elena Simoni; Vincenzo Tumiatti; Carlo Melchiorre
Multitarget-directed ligands: innovative chemical probes and therapeutic tools against Alzheimer's disease.
Current topics in medicinal chemistry 2011;11(22):2797-806.
2011: Michela Rosini; Elena Simoni; Andrea Tarozzi; Andrea Milelli; Vincenza Andrisano; Manuela Bartolini; Maria Laura Bolognesi; Patrizia Hrelia; Riccardo Matera; Carlo Melchiorre
Exploiting the lipoic acid structure in the search for novel multitarget ligands against Alzheimer's disease.
European journal of medicinal chemistry 2011;46(11):5435-42.
2011: Maria Laura Bolognesi; Manuela Bartolini; Andrea Tarozzi; Fabiana Morroni; Federica Lizzi; Andrea Milelli; Anna Minarini; Michela Rosini; Patrizia Hrelia; Vincenza Andrisano; Carlo Melchiorre
Multitargeted drugs discovery: balancing anti-amyloid and anticholinesterase capacity in a single chemical entity.
Bioorganic & medicinal chemistry letters 2011;21(9):2655-8.
2010: Gianni Sagratini; Piero Angeli; Michela Buccioni; Ugo Gulini; Gabriella Marucci; Carlo Melchiorre; Elena Poggesi; Dario Giardinà
Synthesis and α1-adrenoceptor antagonist activity of tamsulosin analogues.
European journal of medicinal chemistry 2010;45(12):5800-7.
2010: Elena Simoni; Christian Bergamini; Romana Fato; Andrea Tarozzi; Sandip Bains; Roberto Motterlini; Andrea Cavalli; Maria Laura Bolognesi; Anna Minarini; Patrizia Hrelia; Giorgio Lenaz; Michela Rosini; Carlo Melchiorre
Polyamine conjugation of curcumin analogues toward the discovery of mitochondria-directed neuroprotective agents.
Journal of medicinal chemistry 2010;53(19):7264-8.
2010: Carlo Melchiorre; Maria Laura Bolognesi; Anna Minarini; Michela Rosini; Vincenzo Tumiatti
Polyamines in drug discovery: from the universal template approach to the multitarget-directed ligand design strategy.
Journal of medicinal chemistry 2010;53(16):5906-14.
2010: Maria Laura Bolognesi; Manuela Bartolini; Francesca Mancini; Gianpaolo Chiriano; Luisa Ceccarini; Michela Rosini; Andrea Milelli; Vincenzo Tumiatti; Vincenza Andrisano; Carlo Melchiorre
Bis(7)-tacrine derivatives as multitarget-directed ligands: Focus on anticholinesterase and antiamyloid activities.
ChemMedChem 2010;5(8):1215-20.
2010: Anna Minarini; Andrea Milelli; Vincenzo Tumiatti; Michela Rosini; Maria Laura Bolognesi; Carlo Melchiorre
Synthetic polyamines: an overview of their multiple biological activities.
Amino acids 2010;38(2):383-92.
2010: Vincenzo Tumiatti; Anna Minarini; Maria Laura Bolognesi; A Milelli; Michela Rosini; Carlo Melchiorre
Tacrine derivatives and Alzheimer's disease.
Current medicinal chemistry 2010;17(17):1825-38.
2009: Vincenzo Tumiatti; Andrea Milelli; Anna Minarini; Marialuisa Micco; Anna Gasperi-Campani; Laura Roncuzzi; Daniela Baiocchi; Jessica Marinello; Giovanni Capranico; Maddalena Zini; Claudio Stefanelli; Carlo Melchiorre
Design, synthesis, and biological evaluation of substituted naphthalene imides and diimides as anticancer agent.
Journal of medicinal chemistry 2009;52(23):7873-7.
2009: Maria Laura Bolognesi; Andrea Cavalli; Christian Bergamini; Romana Fato; Giorgio Lenaz; Michela Rosini; Manuela Bartolini; Vincenza Andrisano; Carlo Melchiorre
Toward a rational design of multitarget-directed antioxidants: merging memoquin and lipoic acid molecular frameworks.
Journal of medicinal chemistry 2009;52(23):7883-6.
2009: Maddalena Zini; Catherine L Passariello; Davide Gottardi; Silvia Cetrullo; Flavio Flamigni; Carla Pignatti; Anna Minarini; Vincenzo Tumiatti; Andrea Milelli; Carlo Melchiorre; Claudio Stefanelli
Cytotoxicity of methoctramine and methoctramine-related polyamines.
Chemico-biological interactions 2009;181(3):409-16.
2009: Francesca Mancini; Maria Laura Bolognesi; Carlo Melchiorre; Vincenza Andrisano
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.
2009: Dario Giardinà; Daniele Martarelli; Gianni Sagratini; Piero Angeli; Dario Ballinari; Ugo Gulini; Carlo Melchiorre; Elena Poggesi; Pierluigi Pompei
Doxazosin-related alpha1-adrenoceptor antagonists with prostate antitumor activity.
Journal of medicinal chemistry 2009;52(15):4951-4.
2009: Maria Laura Bolognesi; Manuela Bartolini; Michela Rosini; Vincenza Andrisano; Carlo Melchiorre
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.
2009: Maria L Bolognesi; Riccardo Matera; Anna Minarini; Michela Rosini; Carlo Melchiorre
Alzheimer's disease: new approaches to drug discovery.
Current opinion in chemical biology 2009;13(3):303-8.
2009: Maria Laura Bolognesi; Michela Rosini; Vincenza Andrisano; Manuela Bartolini; Anna Minarini; Vincenzo Tumiatti; Carlo Melchiorre
MTDL design strategy in the context of Alzheimer's disease: from lipocrine to memoquin and beyond.
Current pharmaceutical design 2009;15(6):601-13.
2009: Maria Laura Bolognesi; Andrea Cavalli; Carlo Melchiorre
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.
2008: Vincenzo Tumiatti; Andrea Milelli; Anna Minarini; Michela Rosini; Maria Laura Bolognesi; Marialuisa Micco; Vincenza Andrisano; Manuela Bartolini; Francesca Mancini; Maurizio Recanatini; Andrea Cavalli; Carlo Melchiorre
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.
2008: Maria Laura Bolognesi; Natalia Calonghi; Chiara Mangano; Lanfranco Masotti; Carlo Melchiorre
Parallel synthesis and cytotoxicity evaluation of a polyamine-quinone conjugates library.
Journal of medicinal chemistry 2008;51(17):5463-7.
2008: Maria Laura Bolognesi; Anna Minarini; Michela Rosini; Vincenzo Tumiatti; Carlo Melchiorre
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.
2008: Michela Rosini; Elena Simoni; Manuela Bartolini; Andrea Cavalli; Luisa Ceccarini; Nicoleta Pascu; David W McClymont; Andrea Tarozzi; Maria L Bolognesi; Anna Minarini; Vincenzo Tumiatti; Vincenza Andrisano; Ian R Mellor; Carlo Melchiorre
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.
2008: Anna Minarini; Gabriella Marucci; Cristina Bellucci; Gianluca Giorgi; Vincenzo Tumiatti; Maria Laura Bolognesi; Riccardo Matera; Michela Rosini; Carlo Melchiorre
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.
2008: Andrea Cavalli; Maria Laura Bolognesi; Anna Minarini; Michela Rosini; Vincenzo Tumiatti; Maurizio Recanatini; Carlo Melchiorre
Multi-target-directed ligands to combat neurodegenerative diseases.
Journal of medicinal chemistry 2008;51(3):347-72.
2007: Maria Laura Bolognesi; Andrea Cavalli; Luca Valgimigli; Manuela Bartolini; Michela Rosini; Vincenza Andrisano; Maurizio Recanatini; Carlo Melchiorre
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.
2007: Manuela Bartolini; Carlo Bertucci; Maria Laura Bolognesi; Andrea Cavalli; Carlo Melchiorre; Vincenza Andrisano
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.
2007: Francesca Mancini; Maria Laura Bolognesi; Carlo Melchiorre; Andrea Cavalli; Vincenza Andrisano
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.
2007: Maria Laura Bolognesi; Rita Banzi; Manuela Bartolini; Andrea Cavalli; Andrea Tarozzi; Vincenza Andrisano; Anna Minarini; Michela Rosini; Vincenzo Tumiatti; Christian Bergamini; Romana Fato; Giorgio Lenaz; Patrizia Hrelia; Antonino Cattaneo; Maurizio Recanatini; Carlo Melchiorre
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.
2007: Vincenzo Tumiatti; Anna Minarini; Andrea Milelli; Michela Rosini; Michela Buccioni; Gabriella Marucci; Carla Ghelardini; Cristina Bellucci; Carlo Melchiorre
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.
2007: Gianni Sagratini; Piero Angeli; Michela Buccioni; Ugo Gulini; Gabriella Marucci; Carlo Melchiorre; Amedeo Leonardi; Elena Poggesi; Dario Giardinà
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.
2007: Natalia Calonghi; Eleonora Pagnotta; Carola Parolin; C Mangano; M L Bolognesi; Carlo Melchiorre; Lanfranco Masotti
A new EGFR inhibitor induces apoptosis in colon cancer cells.
Biochemical and biophysical research communications 2007;354(2):409-13.
2007: Andrea Cavalli; Maria Laura Bolognesi; Simona Capsoni; Vincenza Andrisano; Manuela Bartolini; Elisa Margotti; Antonino Cattaneo; Maurizio Recanatini; Carlo Melchiorre
A small molecule targeting the multifactorial nature of Alzheimer's disease.
Angewandte Chemie (International ed. in English) 2007;46(20):3689-92.
2007: Michela Rosini; Maria Laura Bolognesi; Dario Giardinà; Anna Minarini; Vincenzo Tumiatti; Carlo Melchiorre
Recent advances in alpha1-adrenoreceptor antagonists as pharmacological tools and therapeutic agents.
Current topics in medicinal chemistry 2007;7(2):147-62.
2006: Michela Rosini; Francesca Mancini; Andrea Tarozzi; Francesco Colizzi; Vincenza Andrisano; Maria Laura Bolognesi; Patrizia Hrelia; Carlo Melchiorre
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.
2006: Alessandra Antonello; Andrea Tarozzi; Fabiana Morroni; Andrea Cavalli; Michela Rosini; Patrizia Hrelia; Maria Laura Bolognesi; Carlo Melchiorre
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.
2006: Maria Laura Bolognesi; Anna Minarini; Vincenzo Tumiatti; Carlo Melchiorre
Lipoic acid, a lead structure for multi-target-directed drugs for neurodegeneration.
Mini reviews in medicinal chemistry 2006;6(11):1269-74.
2006: Anna Minarini; Vincenzo Tumiatti; Maria Laura Bolognesi; Carlo Melchiorre
Recent advances in the design and synthesis of prazosin derivatives.
Expert opinion on drug discovery 2006;1(5):395-407.
2005: Gabriella Marucci; Piero Angeli; Michela Buccioni; Ugo Gulini; Carlo Melchiorre; Gianni Sagratini; Rodolfo Testa; Dario Giardinà
(+)-Cyclazosin, a selective alpha1B-adrenoceptor antagonist: functional evaluation in rat and rabbit tissues.
European journal of pharmacology 2005;522(1-3):100-7.
2005: Maria Laura Bolognesi; Vincenza Andrisano; Manuela Bartolini; Andrea Cavalli; Anna Minarini; Maurizio Recanatini; Michela Rosini; Vincenzo Tumiatti; Carlo Melchiorre
Heterocyclic inhibitors of AChE acylation and peripheral sites.
Farmaco (Società chimica italiana : 1989) 2005;60(6-7):465-73.
2005: Michela Rosini; Vincenza Andrisano; Manuela Bartolini; Maria Laura Bolognesi; Patrizia Hrelia; Anna Minarini; Andrea Tarozzi; Carlo Melchiorre
Rational approach to discover multipotent anti-Alzheimer drugs.
Journal of medicinal chemistry 2005;48(2):360-3.
2005: Alessandra Antonello; Patrizia Hrelia; Amedeo Leonardi; Gabriella Marucci; Michela Rosini; Andrea Tarozzi; Vincenzo Tumiatti; Carlo Melchiorre
Design, synthesis, and biological evaluation of prazosin-related derivatives as multipotent compounds.
Journal of medicinal chemistry 2005;48(1):28-31.
2005: Maria Laura Bolognesi; Vincenza Andrisano; Manuela Bartolini; Rita Banzi; Carlo Melchiorre
Propidium-based polyamine ligands as potent inhibitors of acetylcholinesterase and acetylcholinesterase-induced amyloid-beta aggregation.
Journal of medicinal chemistry 2005;48(1):24-7.
2004: Vincenzo Tumiatti; Vincenza Andrisano; Rita Banzi; Manuela Bartolini; Anna Minarini; Michela Rosini; Carlo Melchiorre
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.
2004: Dario Giardinà; Gianni Sagratini; Massimo Grelli; Ugo Gulini; Carlo Melchiorre; Luciano Antolini
Absolute configuration of the alpha (1B)-adrenoceptor antagonist (+)-cyclazosin.
Farmaco (Società chimica italiana : 1989) 2004;59(12):965-9.
2004: Ian R Mellor; Jane Ogilvie; Florentina Pluteanu; Richard H Clothier; Terence L Parker; Michela Rosini; Anna Minarini; Vincenzo Tumiatti; Carlo Melchiorre
Methoctramine analogues inhibit responses to capsaicin and protons in rat dorsal root ganglion neurons.
European journal of pharmacology 2004;505(1-3):37-50.
2004: Maria Laura Bolognesi; Manuela Bartolini; Andrea Cavalli; Vincenza Andrisano; Michela Rosini; Anna Minarini; Carlo Melchiorre
Design, synthesis, and biological evaluation of conformationally restricted rivastigmine analogues.
Journal of medicinal chemistry 2004;47(24):5945-52.
2003: Michela Rosini; Alessandra Antonello; Andrea Cavalli; Maria Laura Bolognesi; Anna Minarini; Gabriella Marucci; Elena Poggesi; Amedeo Leonardi; Carlo Melchiorre
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.
2003: Maria Laura Bolognesi; Andrea Cavalli; Vincenza Andrisano; Manuela Bartolini; Rita Banzi; Alessandra Antonello; Michela Rosini; Carlo Melchiorre
Design, synthesis and biological evaluation of ambenonium derivatives as AChE inhibitors.
Farmaco (Società chimica italiana : 1989) 2003;58(9):917-28.
2003: Dario Giardinà; O Polimanti; Gianni Sagratini; Piero Angeli; Ugo Gulini; Gabriella Marucci; Carlo Melchiorre; Elena Poggesi; Amedeo Leonardi
Searching for cyclazosin analogues as alpha(1B)-adrenoceptor antagonists.
Farmaco (Società chimica italiana : 1989) 2003;58(7):477-87.
2003: Vincenzo Tumiatti; Michela Rosini; Manuela Bartolini; Andrea Cavalli; Gabriella Marucci; Vincenza Andrisano; Piero Angeli; Rita Banzi; Anna Minarini; Maurizio Recanatini; Carlo Melchiorre
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.
2003: Carlo Melchiorre; Alessandra Antonello; Rita Banzi; Maria Laura Bolognesi; Anna Minarini; Michela Rosini; Vincenzo Tumiatti
Polymethylene tetraamine backbone as template for the development of biologically active polyamines.
Medicinal research reviews 2003;23(2):200-33.
2002: Maria Laura Bolognesi; M Gabriele Bixel; Gabriella Marucci; Manuela Bartolini; Michael Krauss; Piero Angeli; Alessandra Antonello; Michela Rosini; Vincenzo Tumiatti; Ferdinand Hucho; Carlo Melchiorre
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.
2002: Dario Giardinà; Mauro Crucianelli; Piero Angeli; Michela Buccioni; Ugo Gulini; Gabriella Marucci; Gianni Sagratini; Carlo Melchiorre
Structure--activity relationships among novel phenoxybenzamine-related beta-chloroethylamines.
Bioorganic & medicinal chemistry 2002;10(5):1291-303.
2002: Michela Rosini; M Gabriele Bixel; Gabriella Marucci; Roberta Budriesi; Michael Krauss; Maria Laura Bolognesi; Anna Minarini; Vincenzo Tumiatti; Ferdinand Hucho; Carlo Melchiorre
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.
2002: Wilma Quaglia; Maria Pigini; Alessandro Piergentili; Mario Giannella; Francesco Gentili; Gabriella Marucci; Antonio Carrieri; Angelo Carotti; Elena Poggesi; Amedeo Leonardi; Carlo Melchiorre
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.
2001: Carlo Melchiorre; Maria Laura Bolognesi; Roberta Budriesi; Carla Ghelardini; Alberto Chiarini; Anna Minarini; Michela Rosini; Vincenzo Tumiatti; E J Wade
Design, synthesis, and biological activity of methoctramine-related polyamines as putative G(i) protein activators.
Journal of medicinal chemistry 2001;44(24):4035-8.
2001: M Gabriele Bixel; Christoph Weise; Maria Laura Bolognesi; Michela Rosini; M J Brierly; Ian R Mellor; Peter N R Usherwood; Carlo Melchiorre; Ferdinand Hucho
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.
2001: Roberta Budriesi; S Cacciaguerra; R D Toro; Maria Laura Bolognesi; Alberto Chiarini; Anna Minarini; Michela Rosini; santi spampinato; Vincenzo Tumiatti; Carlo Melchiorre
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.
2001: Maria Laura Bolognesi; Gabriella Marucci; Piero Angeli; Michela Buccioni; Anna Minarini; Michela Rosini; Vincenzo Tumiatti; Carlo Melchiorre
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.
2001: Maria Laura Bolognesi; Vincenza Andrisano; Manuela Bartolini; Anna Minarini; Michela Rosini; Vincenzo Tumiatti; Carlo Melchiorre
Hexahydrochromeno[4,3-b]pyrrole derivatives as acetylcholinesterase inhibitors.
Journal of medicinal chemistry 2001;44(1):105-9.
2001: M Gabriele Bixel; Michael Krauss; Christoph Weise; Maria Laura Bolognesi; Michela Rosini; Peter N R Usherwood; Carlo Melchiorre; Ferdinand Hucho
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.
2001: Y Li; K Popaj; M Lochner; H Geneste; Roberta Budriesi; Alberto Chiarini; Carlo Melchiorre; Manfred Hesse
Analogues of polyamine alkaloids and their synthetic advantages.
Farmaco (Società chimica italiana : 1989) 2001;56(1-2):127-31.
2000: Vincenzo Tumiatti; Piero Angeli; Vincenza Andrisano; Maria Laura Bolognesi; Andrea Cavalli; Gabriella Marucci; Anna Minarini; Maurizio Recanatini; Michela Rosini; Carlo Melchiorre
[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.
2000: Carlo Melchiorre; Piero Angeli; Maria Laura Bolognesi; Alberto Chiarini; Dario Giardinà; Ugo Gulini; Amedeo Leonardi; Gabriella Marucci; Anna Minarini; Maria Pigini; Wilma Quaglia; Michela Rosini; Vincenzo Tumiatti
Alpha 1-adrenoreceptor antagonists bearing a quinazoline or a benzodioxane moiety.
Pharmaceutica acta Helvetiae 2000;74(2-3):181-90.
2000: Gianluigi D'Agostino; M L Bolognesi; Adele Lucchelli; D Vicini; Barbara Balestra; V Spelta; Carlo Melchiorre; Marcello Tonini
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.
2000: M Gabriele Bixel; Michael Krauss; Y Liu; Maria Laura Bolognesi; Michela Rosini; I S Mellor; Peter N R Usherwood; Carlo Melchiorre; K Nakanishi; Ferdinand Hucho
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.
1999: Michela Rosini; Roberta Budriesi; M Gabriele Bixel; Maria Laura Bolognesi; Alberto Chiarini; Ferdinand Hucho; P Krogsgaard-Larsen; Ian R Mellor; Anna Minarini; Vincenzo Tumiatti; Peter N R Usherwood; Carlo Melchiorre
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.
1999: Maria Laura Bolognesi; Roberta Budriesi; Andrea Cavalli; Alberto Chiarini; Roberto Gotti; Amedeo Leonardi; Anna Minarini; Elena Poggesi; Maurizio Recanatini; Michela Rosini; Vincenzo Tumiatti; Carlo Melchiorre
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.
1999: Wilma Quaglia; Maria Pigini; Alessandro Piergentili; Mario Giannella; Gabriella Marucci; Elena Poggesi; Amedeo Leonardi; Carlo Melchiorre
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.
1998: Maria Laura Bolognesi; Roberta Budriesi; Alberto Chiarini; Elena Poggesi; Amedeo Leonardi; Carlo Melchiorre
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.
1998: Carlo Melchiorre; Vincenza Andrisano; Maria Laura Bolognesi; Roberta Budriesi; Andrea Cavalli; Vanni Cavrini; Michela Rosini; Vincenzo Tumiatti; Maurizio Recanatini
Acetylcholinesterase noncovalent inhibitors based on a polyamine backbone for potential use against Alzheimer's disease.
Journal of medicinal chemistry 1998;41(22):4186-9.
1998: Maria Laura Bolognesi; Anna Minarini; Roberta Budriesi; S Cacciaguerra; Alberto Chiarini; santi spampinato; Vincenzo Tumiatti; Carlo Melchiorre
Universal template approach to drug design: polyamines as selective muscarinic receptor antagonists.
Journal of medicinal chemistry 1998;41(21):4150-60.
1998: Pascaline VAEZ-OLIVERA; A Colelli; M L Bolognesi; Anna Minarini; Vincenzo Tumiatti; Giovanni U Corsini; Carlo Melchiorre; Roberto Maggio
Antagonist binding profile of the split chimeric muscarinic m2-trunc/m3-tail receptor.
European journal of pharmacology 1998;355(2-3):267-74.
1998: Anna Minarini; Roberta Budriesi; Alberto Chiarini; Amedeo Leonardi; Carlo Melchiorre
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.
1998: Wilma Quaglia; Mario Giannella; Alessandro Piergentili; Maria Pigini; Livio Brasili; Rosanna Di Toro; L Rossetti; santi spampinato; Carlo Melchiorre
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.
1998: Carlo Melchiorre; Maria Laura Bolognesi; Roberta Budriesi; Alberto Chiarini; Dario Giardinà; Anna Minarini; Wilma Quaglia; Amedeo Leonardi
Search for selective antagonists at alpha 1-adrenoreceptors: neutral or negative antagonism?
Farmaco (Società chimica italiana : 1989) 1998;53(4):278-86.
1997: Dario Giardinà; M Crucianelli; Gabriella Marucci; Piero Angeli; Carlo Melchiorre; Luciano Antolini
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.
1996: Dario Giardinà; M Crucianelli; R Romanelli; Amedeo Leonardi; Elena Poggesi; Carlo Melchiorre
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.
1996: Dario Giardinà; M Crucianelli; Gabriella Marucci; Carlo Melchiorre; C Polidori; Pierluigi Pompei; M Massi
Pharmacological evaluation of prazosin- and doxazosin-related compounds with modified piperazine ring.
Arzneimittel-Forschung 1996;46(11):1054-9.
1996: Wilma Quaglia; Maria Pigini; Seyed Khosrow Tayebati; Alessandro Piergentili; Mario Giannella; Amedeo Leonardi; C Taddei; Carlo Melchiorre
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.
1996: Wilma Quaglia; Mario Giannella; Gabriella Marucci; Alessandro Piergentili; Maria Pigini; Seyed Khosrow Tayebati; Carlo Melchiorre
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.
1995: Dario Giardinà; M Crucianelli; Carlo Melchiorre; C Taddei; R Testa
Receptor binding profile of cyclazosin, a new alpha 1B-adrenoceptor antagonist.
European journal of pharmacology 1995;287(1):13-6.
1995: Piero Angeli; Franco Cantalamessa; U Gulini; Carlo Melchiorre
Selective blockade of muscarinic M2 receptors in vivo by the new antagonist tripitramine.
Naunyn-Schmiedeberg's archives of pharmacology 1995;352(3):304-7.
1995: Alberto Chiarini; Roberta Budriesi; M L Bolognesi; Anna Minarini; Carlo Melchiorre
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.
1995: Maurizio Recanatini; Vincenzo Tumiatti; Roberta Budriesi; Alberto Chiarini; P Sabatino; M L Bolognesi; Carlo Melchiorre
Synthesis, muscarinic blocking activity and molecular modeling studies of 4-DAMP-related compounds.
Bioorganic & medicinal chemistry 1995;3(3):267-77.
1995: Carlo Melchiorre; Anna Minarini; Roberta Budriesi; Alberto Chiarini; santi spampinato; Vincenzo Tumiatti
The design of novel methoctramine-related tetraamines as muscarinic receptor subtype selective antagonists.
Life sciences 1995;56(11-12):837-44.
1995: Dario Giardinà; M Crucianelli; Gabriella Marucci; F Paparelli; Carlo Melchiorre
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.
1994: Carlo Melchiorre; Patrizia Romualdi; M L Bolognesi; A Donatini; S Ferri
Binding profile of benextramine at neuropeptide Y receptor subtypes in rat brain areas.
European journal of pharmacology 1994;265(1-2):93-8.
1994: Anna Minarini; M L Bolognesi; Roberta Budriesi; Marco Canossa; Alberto Chiarini; santi spampinato; Carlo Melchiorre
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.
1994: Roberto Maggio; Pascaline VAEZ-OLIVERA; M L Bolognesi; Anna Minarini; D Tedeschi; Carlo Melchiorre
Binding profile of the selective muscarinic receptor antagonist tripitramine.
European journal of pharmacology 1994;268(3):459-62.
1993: Carlo Melchiorre; M L Bolognesi; Alberto Chiarini; Anna Minarini; santi spampinato
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.
1993: Wilma Quaglia; Maria Pigini; Seyed Khosrow Tayebati; Alessandro Piergentili; Mario Giannella; Gabriella Marucci; Carlo Melchiorre
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.
1993: Dario Giardinà; U Gulini; M Massi; M G Piloni; Pierluigi Pompei; G Rafaiani; Carlo Melchiorre
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.
1992: Maurizio Recanatini; Anna Minarini; Carlo Melchiorre; Roberta Budriesi; M L Bolognesi
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.
1992: Vincenza Andrisano; Gabriella Marucci; Carlo Melchiorre; Vincenzo Tumiatti
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.
1991: Anna Minarini; Roberta Budriesi; Alberto Chiarini; Carlo Melchiorre; Vincenzo Tumiatti
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.
1991: Wilma Quaglia; Dario Giardinà; Gabriella Marucci; Carlo Melchiorre; Anna Minarini; Vincenzo Tumiatti
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.
1990: Dario Giardinà; U Gulini; Maria Pigini; M G Piloni; Carlo Melchiorre
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.
1990: Wilma Quaglia; Maria Pigini; Mario Giannella; Carlo Melchiorre
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.
1990: Alberto Chiarini; Anna Minarini; Roberta Budriesi; Carlo Melchiorre
Molecular properties of the histamine H2-receptor. Covalent inhibition by tetraamine disulfides.
Farmaco (Società chimica italiana : 1989) 1990;45(9):1001-11.
1990: Carlo Melchiorre
Polymethylene tetraamines: a novel class of cardioselective M2-antagonists.
Medicinal research reviews 1990;10(3):327-49.
1989: Carlo Melchiorre; Anna Minarini; Piero Angeli; Dario Giardinà; U Gulini; Wilma Quaglia
Polymethylene tetraamines as muscarinic receptor probes.
Trends in pharmacological sciences 1989;Suppl():55-9.
1989: Carlo Melchiorre; Wilma Quaglia; M T Picchio; Dario Giardinà; Livio Brasili; Piero Angeli
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.
1989: Dario Giardinà; Livio Brasili; M Gregori; M Massi; M T Picchio; Wilma Quaglia; Carlo Melchiorre
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.
1988: Carlo Melchiorre; Dario Giardinà; U Gulini; Maria Pigini; Wilma Quaglia
Benzodioxanes and quinazolines: probes for characterizing alpha-adrenoreceptors.
Il Farmaco; edizione scientifica 1988;43(12 Suppl):1141-52.
1988: Maria Pigini; Livio Brasili; Mario Giannella; Dario Giardinà; U Gulini; Wilma Quaglia; Carlo Melchiorre
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.
1988: Wilma Quaglia; Livio Brasili; G Cristalli; Dario Giardinà; M T Picchio; Carlo Melchiorre
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.
1988: Carlo Melchiorre; A Cassinelli; Livio Brasili; Dario Giardinà; U Gulini; Wilma Quaglia
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.
1987: Carlo Melchiorre; Piero Angeli; G Lambrecht; E Mutschler; M T Picchio; J Wess
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.
1987: Carlo Melchiorre; A Cassinelli; Wilma Quaglia
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.
1986: M Massi; F Venturi; Livio Brasili; Carlo Melchiorre
Hypotensive effect in dogs and rats of intravenous injections of the alpha 1-adrenoreceptor antagonist benoxathian.
Pharmacological research communications 1986;18(9):813-29.
1986: Livio Brasili; A Cassinelli; P Angeli; Carlo Melchiorre
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.
1985: Piero Angeli; Livio Brasili; E Brancia; Dario Giardinà; Wilma Quaglia; Carlo Melchiorre
Structure-activity relationships among benextramine-related tetraamine disulfides at peripheral alpha-adrenoreceptors.
Journal of medicinal chemistry 1985;28(11):1643-7.
1985: Dario Giardinà; R Bertini; E Brancia; Livio Brasili; Carlo Melchiorre
Structure-activity relationships for prazosin and WB 4101 analogues as alpha 1-adrenoreceptor antagonists.
Journal of medicinal chemistry 1985;28(9):1354-7.
1984: Carlo Melchiorre; Livio Brasili; Dario Giardinà; Maria Pigini; Giovannella Strappaghetti
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.
1984: Livio Brasili; Piero Angeli; E Brancia; Carlo Melchiorre
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.
1983: Carlo Melchiorre; P Gallucci
The irreversible alpha-blocker benextramine interacts with two different thiol groups.
Il Farmaco; edizione scientifica 1983;38(12):950-6.
1982: Carlo Melchiorre; Dario Giardinà; P Gallucci; Livio Brasili
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.
1982: B Belleau; B G Benfey; Carlo Melchiorre; M Montambault
Inhibition of adrenaline-induced platelet aggregation by the alpha-adrenoceptor blocking drug benextramine.
British journal of pharmacology 1982;76(2):253-7.
1982: B Belleau; B G Benfey; Carlo Melchiorre
Presynaptic effect of clonidine antagonized by the tetramine disulphide, benextramine.
British journal of pharmacology 1982;75(4):617-21.
1982: B Belleau; B G Benfey; T J Benfey; Carlo Melchiorre
Inhibition by the tetramine disulphide, benextramine, of cardiac chronotropic histamine H2-receptor-mediated effects.
British journal of pharmacology 1982;75(4):573-8.
1981: Piero Angeli; Livio Brasili; Dario Giardinà; Carlo Melchiorre
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.
1980: Livio Brasili; Carlo Melchiorre; B Belleau; B G Benfey
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.
1980: B G Benfey; B Belleau; Livio Brasili; Mario Giannella; Carlo Melchiorre
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.
1980: B G Benfey; Livio Brasili; Carlo Melchiorre; B Belleau
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.
1980: Mario Giannella; P Angeli; Carlo Melchiorre; Livio Brasili
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.