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Federico Da Settimo

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Chemicals & Drugs

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Elisa Nuti; Elisabetta Orlandini; Silvia Salerno; Salvatore Santamaria; Sabrina Taliani; Kazuhiro Yamamoto; Francesca Casalini; Federico Da Settimo; Valeria La Pietra; Luciana Marinelli; Anna Maria Marini; Hideaki Nagase; Susanna Nencetti; Ettore Novellino; Armando Rossello
Arylsulfonamide inhibitors of aggrecanases as potential therapeutic agents for osteoarthritis: synthesis and biological evaluation.
Stefania Sartini; Francesca Simorini; Sabrina Taliani; Elisabetta Barresi; Sandro Cosconati; Federico Da Settimo; Salvatore Di Maro; Luciana Marinelli; Anna Maria Marini; Ettore Novellino; Silvia Salerno; Concettina La Motta
Benzofuroxane derivatives as multi-effective agents for the treatment of cardiovascular diabetic complications. Synthesis, functional evaluation, and molecular modeling studies.
Anna M Marini; Robert McKenna; Susanna Nencetti; Elisa Nuti; Elisabetta Orlandini; Armando Rossello; Silvia Salerno; Andrea Scozzafava; Francesca Simorini; Mayank Aggarwal; Federico Da Settimo; Concettina La Motta; Alfonso Maresca; Sabrina Taliani; Claudiu T Supuran
Tricyclic sulfonamides incorporating benzothiopyrano[4,3-c]pyrazole and pyridothiopyrano[4,3-c]pyrazole effectively inhibit α- and β-carbonic anhydrase: X-ray crystallography and solution investigations on 15 isoforms.

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All Publications

2013: Elisa Nuti; Elisabetta Orlandini; Silvia Salerno; Salvatore Santamaria; Sabrina Taliani; Kazuhiro Yamamoto; Francesca Casalini; Federico Da Settimo; Valeria La Pietra; Luciana Marinelli; Anna Maria Marini; Hideaki Nagase; Susanna Nencetti; Ettore Novellino; Armando Rossello
Arylsulfonamide inhibitors of aggrecanases as potential therapeutic agents for osteoarthritis: synthesis and biological evaluation.
European journal of medicinal chemistry 2013;62():379-94.
2012: Stefania Sartini; Francesca Simorini; Sabrina Taliani; Elisabetta Barresi; Sandro Cosconati; Federico Da Settimo; Salvatore Di Maro; Luciana Marinelli; Anna Maria Marini; Ettore Novellino; Silvia Salerno; Concettina La Motta
Benzofuroxane derivatives as multi-effective agents for the treatment of cardiovascular diabetic complications. Synthesis, functional evaluation, and molecular modeling studies.
Journal of medicinal chemistry 2012;55(23):10523-31.
2012: Anna M Marini; Robert McKenna; Susanna Nencetti; Elisa Nuti; Elisabetta Orlandini; Armando Rossello; Silvia Salerno; Andrea Scozzafava; Francesca Simorini; Mayank Aggarwal; Federico Da Settimo; Concettina La Motta; Alfonso Maresca; Sabrina Taliani; Claudiu T Supuran
Tricyclic sulfonamides incorporating benzothiopyrano[4,3-c]pyrazole and pyridothiopyrano[4,3-c]pyrazole effectively inhibit α- and β-carbonic anhydrase: X-ray crystallography and solution investigations on 15 isoforms.
Journal of medicinal chemistry 2012;55(22):9619-29.
2012: luca Antonioli; Oriana Awwad; Corrado Blandizzi; Rocchina Colucci; Federico Da Settimo; Concettina La Motta; Marco Tuccori; Matteo Fornai
Adenosine deaminase in the modulation of immune system and its potential as a novel target for treatment of inflammatory disorders.
Current drug targets 2012;13(6):842-62.
2012: Sabrina Castellano; Sandro Cosconati; Barbara Costa; Eleonora Da Pozzo; Sara Bendinelli; Giovanni Greco; Claudia Martini; Ciro Milite; Ettore Novellino; Isabella Pugliesi; Elisa Rizzetto; Gianluca Sbardella; Giorgio Stefancich; Sabrina Taliani; Federico Da Settimo
Synthesis and biological evaluation of 4-phenylquinazoline-2-carboxamides designed as a novel class of potent ligands of the translocator protein.
Journal of medicinal chemistry 2012;55(9):4506-10.
2012: Anna Ramunno; Stefania Sartini; Sara Angiuoli; Sandro Cosconati; Federico Da Settimo; Salvatore Di Maro; Mariateresa Giustiniano; Concettina La Motta; Valeria La Pietra; Vita Maglio; Luciana Marinelli; Ettore Novellino
Progresses in the pursuit of aldose reductase inhibitors: the structure-based lead optimization step.
European journal of medicinal chemistry 2012;51():216-26.
2012: Alessandro Antonelli; Piero Berti; Guido Bocci; Alessandro Corti; Federico Da Settimo; Romano Danesi; Teresa Di Desidero; Andrea Di Domenicantonio; Poupak Fallahi; Silvia Martina Ferrari; Anna Fioravanti; Gabriella Fontanini; Concettina La Motta; Michele N Minuto; Simona Piaggi; Ilaria Ruffilli; Stefania Sartini; Greta Alì; Paolo Miccoli
CLM94, a novel cyclic amide with anti-VEGFR-2 and antiangiogenic properties, is active against primary anaplastic thyroid cancer in vitro and in vivo.
The Journal of clinical endocrinology and metabolism 2012;97(4):E528-36.
2012: Sabrina Taliani; Maria Letizia Trincavelli; Elisabetta Barresi; Sandro Cosconati; Barbara Cosimelli; Simona Daniele; Salvatore Di Maro; Giovanni Greco; Concettina La Motta; Luciana Marinelli; Anna Maria Marini; Claudia Martini; Ettore Novellino; Isabella Pugliesi; Silvia Salerno; Francesca Simorini; Federico Da Settimo
3-aryl-[1,2,4]triazino[4,3-a]benzimidazol-4(10H)-one: a novel template for the design of highly selective A₂B adenosine receptor antagonists.
Journal of medicinal chemistry 2012;55(4):1490-9.
2012: Vittorio Limongelli; Luciana Marinelli; Laura Mugnaini; Ettore Novellino; Sandro Cosconati; Federico Da Settimo; Concettina La Motta; Stefania Sartini; Michele Parrinello
Sampling protein motion and solvent effect during ligand binding.
Proceedings of the National Academy of Sciences of the United States of America 2012;109(5):1467-72.
2012: A Martelli; Lara Testai; M C Breschi; Federico Da Settimo; A Marino; V Calderone
Hydrogen sulphide: biopharmacological roles in the cardiovascular system and pharmaceutical perspectives.
Current medicinal chemistry 2012;19(20):3325-36.
2012: Stefania Sartini; Francesca Simorini; Sabrina Taliani; Federico Da Settimo; Anna Maria Marini; M Morelli; Silvia Salerno; Concettina La Motta
Geometrically constrained derivatives of indolylglyoxylamides as ligands binding the GABAA/BzR complex.
Current topics in medicinal chemistry 2012;12(4):312-20.
2012: Francesca Simorini; Sabrina Taliani; Concettina La Motta; Anna Maria Marini; Isabella Pugliesi; Silvia Salerno; Federico Da Settimo
Medicinal chemistry of indolylglyoxylamide TSPO high affinity ligands with anxiolytic-like effects.
Current topics in medicinal chemistry 2012;12(4):333-51.
2012: Silvia Salerno; Francesca Simorini; Sabrina Taliani; Federico Da Settimo; Giacomo Fornaciari; Concettina La Motta; Anna Maria Marini
Medicinal chemistry of indolylglyoxylamide GABAA/BzR high affinity ligands: identification of novel anxiolytic/non sedative agents.
Current topics in medicinal chemistry 2012;12(4):286-311.
2012: Sabrina Taliani; Federico Da Settimo
The indolylglyoxylamide scaffold as an useful tool to obtain anxiolytic agents.
Current topics in medicinal chemistry 2012;12(4):236-7.
2012: Valeria La Pietra; Concettina La Motta; Luciana Marinelli; Matteo Morelli; Hideaki Nagase; Francesca Casalini; Sandro Cosconati; Federico Da Settimo; Francesco Saverio Di Leva; Elisa Nuti; Isabella Pugliesi; Armando Rossello; Salvatore Santamaria; Sabrina Taliani; Robert Visse; Ettore Novellino
Identification of novel molecular scaffolds for the design of MMP-13 inhibitors: a first round of lead optimization.
European journal of medicinal chemistry 2012;47(1):143-52.
2011: Barbara Cosimelli; Federico Da Settimo; Simona Daniele; Matteo Fornai; Giovanni Greco; Concettina La Motta; Ettore Novellino; Isabella Pugliesi; Annalisa Sala; Elda Severi; Sabrina Taliani; Maria Letizia Trincavelli; luca Antonioli; Corrado Blandizzi; Rocchina Colucci; Claudia Martini
Derivatives of benzimidazol-2-ylquinoline and benzimidazol-2-ylisoquinoline as selective A1 adenosine receptor antagonists with stimulant activity on human colon motility.
ChemMedChem 2011;6(10):1909-18.
2011: Alessia Scatena; Sabrina Taliani; Maria Letizia Trincavelli; Sandro Cosconati; Simona Daniele; Francesco Fornai; Claudia Martini; Isabella Pugliesi; Federico Da Settimo
3-(Fur-2-yl)-10-(2-phenylethyl)-[1,2,4]triazino[4,3-a]benzimidazol-4(10H)-one, a novel adenosine receptor antagonist with A(2A)-mediated neuroprotective effects.
ACS chemical neuroscience 2011;2(9):526-35.
2011: Barbara Cosimelli; Barbara Costa; Eleonora Da Pozzo; Federico Da Settimo; Giovanni Greco; Concettina La Motta; Ettore Novellino; Elda Severi; Francesca Simorini; Sabrina Taliani; Sara Bendinelli; Claudia Martini
Tertiary amides with a five-membered heteroaromatic ring as new probes for the translocator protein.
European journal of medicinal chemistry 2011;46(9):4506-20.
2011: Elisa Nuti; Francesca Casalini; Salvatore Santamaria; Pamela Gabelloni; Sara Bendinelli; Eleonora Da Pozzo; Barbara Costa; Luciana Marinelli; Valeria La Pietra; Ettore Novellino; M Margarida Bernardo; Rafael Fridman; Federico Da Settimo; Claudia Martini; Armando Rossello
Synthesis and biological evaluation in U87MG glioma cells of (ethynylthiophene)sulfonamido-based hydroxamates as matrix metalloproteinase inhibitors.
European journal of medicinal chemistry 2011;46(7):2617-29.
2011: Guido Bocci; Anna Fioravanti; Concettina La Motta; Paola Orlandi; Bastianina Canu; Teresa Di Desidero; Laura Mugnaini; Stefania Sartini; Sandro Cosconati; Rita Frati; Alessandro Antonelli; Piero Berti; Paolo Miccoli; Federico Da Settimo; Romano Danesi
Antiproliferative and proapoptotic activity of CLM3, a novel multiple tyrosine kinase inhibitor, alone and in combination with SN-38 on endothelial and cancer cells.
Biochemical pharmacology 2011;81(11):1309-16.
2011: Simona Rapposelli; Stefania Sartini; Federico Da Settimo; Maria Digiacomo; Concettina La Motta; Annalina Lapucci; Michael Vanni
Synthesis and biological evaluation of 2'-oxo-2,3-dihydro-3'H- spiro[chromene-4,5'-[1,3]oxazolidin]-3'yl]acetic acid derivatives as aldose reductase inhibitors.
Archiv der Pharmazie 2011;344(6):372-85.
2011: Barbara Costa; Eleonora Da Pozzo; Beatrice Chelli; Nicola Simola; Micaela Morelli; Michele Luisi; Marco Maccheroni; Sabrina Taliani; Francesca Simorini; Federico Da Settimo; Claudia Martini
Anxiolytic properties of a 2-phenylindolglyoxylamide TSPO ligand: Stimulation of in vitro neurosteroid production affecting GABAA receptor activity.
Psychoneuroendocrinology 2011;36(4):463-72.
2011: Alessandro Antonelli; Guido Bocci; Concettina La Motta; Silvia Martina Ferrari; Poupak Fallahi; Anna Fioravanti; Stefania Sartini; Michele N Minuto; Simona Piaggi; Alessandro Corti; Greta Alì; Piero Berti; Gabriella Fontanini; Romano Danesi; Federico Da Settimo; Paolo Miccoli
Novel pyrazolopyrimidine derivatives as tyrosine kinase inhibitors with antitumoral activity in vitro and in vivo in papillary dedifferentiated thyroid cancer.
The Journal of clinical endocrinology and metabolism 2011;96(2):E288-96.
2011: Victor W Pike; Isabella Pugliesi; Eugenii A Rabiner; Sabrina Taliani; Sami S Zoghbi; Eleonora Da Pozzo; Masahiro Fujita; Roger Gunn; Jinsoo Hong; Robert B Innis; Talakad G Lohith; Claudia Martini; David R J Owen; Christine A Parker; Federico Da Settimo
Evaluation of novel N1-methyl-2-phenylindol-3-ylglyoxylamides as a new chemotype of 18 kDa translocator protein-selective ligand suitable for the development of positron emission tomography radioligands.
Journal of medicinal chemistry 2011;54(1):366-73.
2011: Stefania Sartini; M Morelli; Federico Da Settimo; B Dario; Concettina La Motta
Receptor tyrosine kinase kit and gastrointestinal stromal tumours: an overview.
Current medicinal chemistry 2011;18(19):2893-903.
2011: Sabrina Taliani; Isabella Pugliesi; Federico Da Settimo
Structural requirements to obtain highly potent and selective 18 kDa Translocator Protein (TSPO) Ligands.
Current topics in medicinal chemistry 2011;11(7):860-86.
2010: luca Antonioli; Matteo Fornai; Rocchina Colucci; Oriana Awwad; Narcisa Ghisu; Marco Tuccori; Federico Da Settimo; Concettina La Motta; Gianfranco Natale; Emiliano Duranti; Agostino Virdis; Corrado Blandizzi
The blockade of adenosine deaminase ameliorates chronic experimental colitis through the recruitment of adenosine A2A and A3 receptors.
The Journal of pharmacology and experimental therapeutics 2010;335(2):434-42.
2010: Sabrina Taliani; Eleonora Da Pozzo; Marusca Bellandi; Sara Bendinelli; Isabella Pugliesi; Francesca Simorini; Concettina La Motta; Silvia Salerno; Anna Maria Marini; Federico Da Settimo; Barbara Cosimelli; Giovanni Greco; Ettore Novellino; Claudia Martini
Novel irreversible fluorescent probes targeting the 18 kDa translocator protein: synthesis and biological characterization.
Journal of medicinal chemistry 2010;53(10):4085-93.
2010: Sabrina Taliani; Concettina La Motta; Laura Mugnaini; Francesca Simorini; Silvia Salerno; Anna Maria Marini; Federico Da Settimo; Sandro Cosconati; Barbara Cosimelli; Giovanni Greco; Vittorio Limongelli; Luciana Marinelli; Ettore Novellino; Osele Ciampi; Simona Daniele; Maria Letizia Trincavelli; Claudia Martini
Novel N2-substituted pyrazolo[3,4-d]pyrimidine adenosine A3 receptor antagonists: inhibition of A3-mediated human glioblastoma cell proliferation.
Journal of medicinal chemistry 2010;53(10):3954-63.
2010: Silvia Salerno; Federico Da Settimo; Sabrina Taliani; Francesca Simorini; Concettina La Motta; G Fornaciari; Anna Maria Marini
Recent advances in the development of dual topoisomerase I and II inhibitors as anticancer drugs.
Current medicinal chemistry 2010;17(35):4270-90.
2010: Sabrina Taliani; Isabella Pugliesi; Marusca Bellandi; Concettina La Motta; Federico Da Settimo
A3 receptor ligands: past, present and future trends.
Current topics in medicinal chemistry 2010;10(10):942-75.
2010: Concettina La Motta; Stefania Sartini; M Morelli; Sabrina Taliani; Federico Da Settimo
Allosteric modulators for adenosine receptors: an alternative to the orthosteric ligands.
Current topics in medicinal chemistry 2010;10(10):976-92.
2009: Tiziano Tuccinardi; Sabrina Taliani; Marusca Bellandi; Federico Da Settimo; Eleonora Da Pozzo; Claudia Martini; Adriano Martinelli
A virtual screening study of the 18 kDa translocator protein using pharmacophore models combined with 3D-QSAR studies.
ChemMedChem 2009;4(10):1686-94.
2009: Sandro Cosconati; Luciana Marinelli; Concettina La Motta; Stefania Sartini; Federico Da Settimo; Arthur J Olson; Ettore Novellino
Pursuing aldose reductase inhibitors through in situ cross-docking and similarity-based virtual screening.
Journal of medicinal chemistry 2009;52(18):5578-81.
2009: Lisa Dalla Via; SM Magno; Ornella Gia; Anna Maria Marini; Federico Da Settimo; Silvia Salerno; Concettina La Motta; Francesca Simorini; Sabrina Taliani; Antonio Lavecchia; Carmen Di Giovanni; Giuseppe Brancato; Vincenzo Barone; Ettore Novellino
Benzothiopyranoindole-based antiproliferative agents: synthesis, cytotoxicity, nucleic acids interaction, and topoisomerases inhibition properties.
Journal of medicinal chemistry 2009;52(17):5429-41.
2009: Sabrina Taliani; Barbara Cosimelli; Federico Da Settimo; Anna Maria Marini; Concettina La Motta; Francesca Simorini; Silvia Salerno; Ettore Novellino; Giovanni Greco; Sandro Cosconati; Luciana Marinelli; F Salvetti; Gianluca L'Abbate; Silvia Trasciatti; Marina Montali; Barbara Costa; Claudia Martini
Identification of anxiolytic/nonsedative agents among indol-3-ylglyoxylamides acting as functionally selective agonists at the gamma-aminobutyric acid-A (GABAA) alpha2 benzodiazepine receptor.
Journal of medicinal chemistry 2009;52(12):3723-34.
2009: Concettina La Motta; Stefania Sartini; Laura Mugnaini; Silvia Salerno; Francesca Simorini; Sabrina Taliani; Anna Maria Marini; Federico Da Settimo; Antonio Lavecchia; Ettore Novellino; luca Antonioli; Matteo Fornai; Corrado Blandizzi; Mario Del Tacca
Exploiting the pyrazolo[3,4-d]pyrimidin-4-one ring system as a useful template to obtain potent adenosine deaminase inhibitors.
Journal of medicinal chemistry 2009;52(6):1681-92.
2009: Concettina La Motta; Stefania Sartini; Tiziano Tuccinardi; Erika Nerini; Federico Da Settimo; Adriano Martinelli
Computational studies of epidermal growth factor receptor: docking reliability, three-dimensional quantitative structure-activity relationship analysis, and virtual screening studies.
Journal of medicinal chemistry 2009;52(4):964-75.
2009: Sabrina Taliani; Federico Da Settimo; Eleonora Da Pozzo; Beatrice Chelli; Claudia Martini
Translocator protein ligands as promising therapeutic tools for anxiety disorders.
Current medicinal chemistry 2009;16(26):3359-80.
2008: Federico Da Settimo; Francesca Simorini; Sabrina Taliani; Concettina La Motta; Anna Maria Marini; Silvia Salerno; Marusca Bellandi; Ettore Novellino; Giovanni Greco; Barbara Cosimelli; Eleonora Da Pozzo; Barbara Costa; Nicola Simola; Micaela Morelli; Claudia Martini
Anxiolytic-like effects of N,N-dialkyl-2-phenylindol-3-ylglyoxylamides by modulation of translocator protein promoting neurosteroid biosynthesis.
Journal of medicinal chemistry 2008;51(18):5798-806.
2008: Concettina La Motta; Stefania Sartini; Silvia Salerno; Francesca Simorini; Sabrina Taliani; Anna Maria Marini; Federico Da Settimo; Luciana Marinelli; Vittorio Limongelli; Ettore Novellino
Acetic acid aldose reductase inhibitors bearing a five-membered heterocyclic core with potent topical activity in a visual impairment rat model.
Journal of medicinal chemistry 2008;51(11):3182-93.
2008: Barbara Cosimelli; Giovanni Greco; Marina Ehlardo; Ettore Novellino; Federico Da Settimo; Sabrina Taliani; Concettina La Motta; Marusca Bellandi; Tiziano Tuccinardi; Adriano Martinelli; Osele Ciampi; Maria Letizia Trincavelli; Claudia Martini
Derivatives of 4-amino-6-hydroxy-2-mercaptopyrimidine as novel, potent, and selective A3 adenosine receptor antagonists.
Journal of medicinal chemistry 2008;51(6):1764-70.
2008: Sabrina Taliani; Federico Da Settimo
Highlighting the new advances in drug discovery and development.
ChemMedChem 2008;3(1):181-4.
2007: Federico Da Settimo; Giampaolo Primofiore; Sabrina Taliani; Anna Maria Marini; Concettina La Motta; Francesca Simorini; Silvia Salerno; Valentina Sergianni; Tiziano Tuccinardi; Adriano Martinelli; Barbara Cosimelli; Giovanni Greco; Ettore Novellino; Osele Ciampi; Maria Letizia Trincavelli; Claudia Martini
5-amino-2-phenyl[1,2,3]triazolo[1,2-a][1,2,4]benzotriazin-1-one: a versatile scaffold to obtain potent and selective A3 adenosine receptor antagonists.
Journal of medicinal chemistry 2007;50(23):5676-84.
2007: Concettina La Motta; Stefania Sartini; Laura Mugnaini; Francesca Simorini; Sabrina Taliani; Silvia Salerno; Anna Maria Marini; Federico Da Settimo; Antonio Lavecchia; Ettore Novellino; Miriam Cantore; Paola Failli; Mario Ciuffi
Pyrido[1,2-a]pyrimidin-4-one derivatives as a novel class of selective aldose reductase inhibitors exhibiting antioxidant activity.
Journal of medicinal chemistry 2007;50(20):4917-27.
2007: luca Antonioli; Matteo Fornai; Rocchina Colucci; Narcisa Ghisu; Federico Da Settimo; Gianfranco Natale; Olga Kastsiuchenka; Emiliano Duranti; Agostino Virdis; Cristina Vassalle; Concettina La Motta; Laura Mugnaini; Maria Cristina Breschi; Corrado Blandizzi; Mario Del Taca
Inhibition of adenosine deaminase attenuates inflammation in experimental colitis.
The Journal of pharmacology and experimental therapeutics 2007;322(2):435-42.
2007: Giampaolo Primofiore; Sabrina Taliani; Federico Da Settimo; Anna Maria Marini; Concettina La Motta; Francesca Simorini; Maria Paola Patrizi; Valentina Sergianni; Ettore Novellino; Giovanni Greco; Barbara Cosimelli; Vincenzo Calderone; Marina Montali; Francois Besnard; Claudia Martini
Novel N-substituted indol-3-ylglyoxylamides probing the LDi and L1/L2 lipophilic regions of the benzodiazepine receptor site in search for subtype-selective ligands.
Journal of medicinal chemistry 2007;50(7):1627-34.
2007: Sabrina Taliani; Francesca Simorini; Valentina Sergianni; Concettina La Motta; Federico Da Settimo; Barbara Cosimelli; Enrico Abignente; Giovanni Greco; Ettore Novellino; Leonardo Rossi; Vittorio Gremigni; Francesca Spinetti; Beatrice Chelli; Claudia Martini
New fluorescent 2-phenylindolglyoxylamide derivatives as probes targeting the peripheral-type benzodiazepine receptor: design, synthesis, and biological evaluation.
Journal of medicinal chemistry 2007;50(2):404-7.
2007: Federico Da Settimo; Sabrina Taliani; Maria Letizia Trincavelli; Marina Montali; Claudia Martini
GABA A/Bz receptor subtypes as targets for selective drugs.
Current medicinal chemistry 2007;14(25):2680-701.
2006: Giampaolo Primofiore; Federico Da Settimo; Anna Maria Marini; Sabrina Taliani; Concettina La Motta; Francesca Simorini; Ettore Novellino; Giovanni Greco; Barbara Cosimelli; Marina Ehlardo; Annalisa Sala; Francois Besnard; Marina Montali; Claudia Martini
Refinement of the benzodiazepine receptor site topology by structure-activity relationships of new N-(heteroarylmethyl)indol-3-ylglyoxylamides.
Journal of medicinal chemistry 2006;49(8):2489-95.
2005: Ettore Novellino; Barbara Cosimelli; Marina Ehlardo; Giovanni Greco; Manuela Iadanza; Antonio Lavecchia; Maria Grazia Rimoli; Annalisa Sala; Antonio Da Settimo; Giampaolo Primofiore; Federico Da Settimo; Sabrina Taliani; Concettina La Motta; Karl-Norbert Klotz; Daniela Tuscano; Maria Letizia Trincavelli; Claudia Martini
2-(Benzimidazol-2-yl)quinoxalines: a novel class of selective antagonists at human A(1) and A(3) adenosine receptors designed by 3D database searching.
Journal of medicinal chemistry 2005;48(26):8253-60.
2005: Federico Da Settimo; Giampaolo Primofiore; Concettina La Motta; Stefania Sartini; Sabrina Taliani; Francesca Simorini; Anna Maria Marini; Antonio Lavecchia; Ettore Novellino; Enrico Boldrini
Naphtho[1,2-d]isothiazole acetic acid derivatives as a novel class of selective aldose reductase inhibitors.
Journal of medicinal chemistry 2005;48(22):6897-907.
2005: Federico Da Settimo; Giampaolo Primofiore; Concettina La Motta; Sabrina Taliani; Francesca Simorini; Anna Maria Marini; Laura Mugnaini; Antonio Lavecchia; Ettore Novellino; Daniela Tuscano; Claudia Martini
Novel, highly potent adenosine deaminase inhibitors containing the pyrazolo[3,4-d]pyrimidine ring system. Synthesis, structure-activity relationships, and molecular modeling studies.
Journal of medicinal chemistry 2005;48(16):5162-74.
2005: Beatrice Chelli; Leonardo Rossi; Eleonora Da Pozzo; Barbara Costa; Francesca Spinetti; Mariarosa Rechichi; Alessandra Salvetti; Annalisa Lena; Francesca Simorini; Renato Vanacore; Fabrizio Scatena; Federico Da Settimo; Vittorio Gremigni; Claudia Martini
PIGA (N,N-Di-n-butyl-5-chloro-2-(4-chlorophenyl)indol-3-ylglyoxylamide), a new mitochondrial benzodiazepine-receptor ligand, induces apoptosis in C6 glioma cells.
Chembiochem : a European journal of chemical biology 2005;6(6):1082-8.
2005: Giampaolo Primofiore; Federico Da Settimo; Sabrina Taliani; Silvia Salerno; Ettore Novellino; Giovanni Greco; Barbara Cosimelli; Francois Besnard; Barbara Costa; Marina Montali; Claudia Martini
High affinity central benzodiazepine receptor ligands: synthesis and biological evaluation of a series of phenyltriazolobenzotriazindione derivatives.
Journal of medicinal chemistry 2005;48(8):2936-43.
2005: Giampaolo Primofiore; Federico Da Settimo; Anna Maria Marini; Francesca Simorini; Concettina La Motta; Sabrina Taliani; Sonia Laneri; Letizia Trincavelli; Claudia Martini
Synthesis and benzodiazepine receptor affinity of derivatives of the new tricyclic heteroaromatic system pyrido[3',2':5,6]thiopyrano[4,3-c]pyridazin-3(2H,5H)-one.
Archiv der Pharmazie 2005;338(2-3):126-32.
2005: Federico Da Settimo; Giampaolo Primofiore; Concettina La Motta; Silvia Salerno; Ettore Novellino; Giovanni Greco; Antonio Lavecchia; Sonia Laneri; Enrico Boldrini
Spirohydantoin derivatives of thiopyrano[2,3-b]pyridin-4(4H)-one as potent in vitro and in vivo aldose reductase inhibitors.
Bioorganic & medicinal chemistry 2005;13(2):491-9.
2004: Giampaolo Primofiore; Federico Da Settimo; Sabrina Taliani; Francesca Simorini; Maria Paola Patrizi; Ettore Novellino; Giovanni Greco; Enrico Abignente; Barbara Costa; Beatrice Chelli; Claudia Martini
N,N-dialkyl-2-phenylindol-3-ylglyoxylamides. A new class of potent and selective ligands at the peripheral benzodiazepine receptor.
Journal of medicinal chemistry 2004;47(7):1852-5.
2003: Giampaolo Primofiore; Federico Da Settimo; Sabrina Taliani; Anna Maria Marini; Francesca Simorini; Ettore Novellino; Giovanni Greco; Letizia Trincavelli; Claudia Martini
Geometrically constrained analogues of N-benzylindolylglyoxylylamides: [1, 2, 4]triazino[4, 3-a]benzimidazol-4(10H)-one derivatives as potential new ligands at the benzodiazepine receptor.
Archiv der Pharmazie 2003;336(9):413-21.
2003: Federico Da Settimo; Giampaolo Primofiore; Antonio Da Settimo; Concettina La Motta; Francesca Simorini; Ettore Novellino; Giovanni Greco; Antonio Lavecchia; Enrico Boldrini
Novel, highly potent aldose reductase inhibitors: cyano(2-oxo-2,3-dihydroindol-3-yl)acetic acid derivatives.
Journal of medicinal chemistry 2003;46(8):1419-28.
2002: Lisa Dalla Via; Ornella Gia; Sebastiano Marciani Magno; Antonio Da Settimo; Giampaolo Primofiore; Federico Da Settimo; Francesca Simorini; Anna Maria Marini
Dialkylaminoalkylindolonaphthyridines as potential antitumour agents: synthesis, cytotoxicity and DNA binding properties.
European journal of medicinal chemistry 2002;37(6):475-86.
2001: Federico Da Settimo; Giampaolo Primofiore; Antonio Da Settimo; Concettina La Motta; Sabrina Taliani; Francesca Simorini; Ettore Novellino; Giovanni Greco; Antonio Lavecchia; Enrico Boldrini
[1,2,4]Triazino[4,3-a]benzimidazole acetic acid derivatives: a new class of selective aldose reductase inhibitors.
Journal of medicinal chemistry 2001;44(25):4359-69.
2001: Lisa Dalla Via; Ornella Gia; SM Magno; Antonio Da Settimo; Anna Maria Marini; Giampaolo Primofiore; Federico Da Settimo; S Salerno
Synthesis, in vitro antiproliferative activity and DNA-interaction of benzimidazoquinazoline derivatives as potential anti-tumor agents.
Farmaco (Società chimica italiana : 1989) 2001;56(3):159-67.
2001: Federico Da Settimo; Giampaolo Primofiore; Sabrina Taliani; Anna Maria Marini; Concettina La Motta; Ettore Novellino; Giovanni Greco; Antonio Lavecchia; Letizia Trincavelli; Claudia Martini
3-Aryl[1,2,4]triazino[4,3-a]benzimidazol-4(10H)-ones: a new class of selective A1 adenosine receptor antagonists.
Journal of medicinal chemistry 2001;44(3):316-27.
2000: Paola Dorigo; Maura Floreani; G Santostasi; I Maragno; Daniela Danieli-Betto; Elena Germinario; SM Magno; Giampaolo Primofiore; Anna Maria Marini; Federico Da Settimo
Pharmacological characterization of a new Ca(2+) sensitizer.
The Journal of pharmacology and experimental therapeutics 2000;295(3):994-1004.
2000: Marco Gesi; Antonio Pellegrini; Paola Lenzi; Federico Da Settimo; Claudia Martini; F Salvetti; Sabrina Taliani; Francesco Fornai
Effects of newly-developed benzodiazepine ligands on noise-induced mitochondrial damage in the rat.
Annals of anatomy = Anatomischer Anzeiger : official organ of the Anatomische Gesellschaft 2000;182(4):311-8.
2000: Giampaolo Primofiore; Federico Da Settimo; Sabrina Taliani; Anna Maria Marini; Concettina La Motta; Ettore Novellino; Giovanni Greco; Marco Gesi; Letizia Trincavelli; Claudia Martini
3-Aryl-[1,2,4]triazino[4,3-a]benzimidazol-4(10H)-ones: tricyclic heteroaromatic derivatives as a new class of benzodiazepine receptor ligands.
Journal of medicinal chemistry 2000;43(1):96-102.
1998: Antonio Da Settimo; Giampaolo Primofiore; Federico Da Settimo; Anna Maria Marini; Ettore Novellino; Giovanni Greco; Marco Gesi; Claudia Martini; Gino Giannaccini; Antonio Lucacchini
N'-Phenylindol-3-ylglyoxylohydrazide derivatives: synthesis, structure-activity relationships, molecular modeling studies, and pharmacological action on brain benzodiazepine receptors.
Journal of medicinal chemistry 1998;41(20):3821-30.
1997: Giampaolo Primofiore; Federico Da Settimo; Concettina La Motta; Francesca Simorini; A Minutolo; Enrico Boldrini
Benzisothiazole-1,1-dioxide alkanoic acid derivatives as inhibitors of rat lens aldose reductase.
Farmaco (Società chimica italiana : 1989) 1997;52(10):583-8.
1997: Antonio Da Settimo; Giampaolo Primofiore; Anna Maria Marini; Federico Da Settimo; V Nuti; Claudia Martini; Letizia Trincavelli; Antonio Lucacchini
Isosteric replacement of amide by ester function. Synthesis and benzodiazepine receptor affinity of indol-3-ylglyoxylyl ester derivatives.
Farmaco (Società chimica italiana : 1989) 1997;52(6-7):421-8.
1996: Antonio Da Settimo; Giampaolo Primofiore; Federico Da Settimo; Anna Maria Marini; E Novellino; G Greco; Claudia Martini; Gino Giannaccini; Antonio Lucacchini
Synthesis, structure-activity relationships, and molecular modeling studies of N-(indol-3-ylglyoxylyl)benzylamine derivatives acting at the benzodiazepine receptor.
Journal of medicinal chemistry 1996;39(26):5083-91.
1996: Federico Da Settimo; Anna Maria Marini; C La Motta; F Simorini; E Luchetti; Simone Bertini
Synthesis and local anaesthetic activity of some 7-amino-2-dialkylaminoalkylpyrrolo[3,4-c]pyridine derivatives.
Farmaco (Società chimica italiana : 1989) 1996;51(11):725-8.
1996: Antonio Da Settimo; Giampaolo Primofiore; C La Motta; Federico Da Settimo; F Simorini; Enrico Boldrini; P Bianchini
Acid derivatives of benzisothiazole-1,1-dioxide as inhibitors of rat lens aldose reductase.
Farmaco (Società chimica italiana : 1989) 1996;51(4):261-7.
1996: Antonio Da Settimo; Giampaolo Primofiore; Federico Da Settimo; E Novellino; G Greco; Claudia Martini; G Senatore; A Lucacehini
Indole derivatives as probes to study the benzodiazepine binding site in GABA receptor complex.
Advances in experimental medicine and biology 1996;398():677-83.
1995: Antonio Da Settimo; Anna Maria Marini; Giampaolo Primofiore; Federico Da Settimo
Synthesis and evaluation of aminoadamantane derivatives for in vitro anti-HIV and antitumor activities.
Farmaco (Società chimica italiana : 1989) 1995;50(5):321-6.
1995: Antonio Da Settimo; Giampaolo Primofiore; Federico Da Settimo; Anna Maria Marini; E Novellino; G Greco; Claudia Martini; G Senatore; Antonio Lucacchini
Synthesis of 3-(2'-furoyl)indole derivatives as potential new ligands at the benzodiazepine receptor, structurally more restrained analogues of indoleglyoxylylamides.
Farmaco (Società chimica italiana : 1989) 1995;50(5):311-20.
1995: Giampaolo Primofiore; Federico Da Settimo; Anna Maria Marini; C La Motta; Claudia Martini; G Senatore; Antonio Lucacchini
N-(indol-3-ylglyoxylyl)amino acid ester derivatives. Synthesis and interaction properties at the benzodiazepine receptor.
Farmaco (Società chimica italiana : 1989) 1995;50(1):5-12.
1994: Antonio Da Settimo; Anna Maria Marini; A M Bianucci; Giampaolo Primofiore; Federico Da Settimo; Enrico Boldrini
Synthesis of 2-methylaminobenzimidazole derivatives tested for antiinflammatory activity.
Farmaco (Società chimica italiana : 1989) 1994;49(12):829-34.
1994: Antonio Da Settimo; Giampaolo Primofiore; Federico Da Settimo; F Simorini; P L Barili; G Senatore; Claudia Martini; Antonio Lucacchini
Synthesis and benzodiazepine receptor activity of some 4,5-dihydro-1H-pyrazolo[4,3-c][1,8]naphthyridine derivatives.
Drug design and discovery 1994;11(4):307-28.
1993: Antonio Da Settimo; Giampaolo Primofiore; Federico Da Settimo; Antonio Lucacchini; Claudia Martini; G Senatore
Benzodiazepine receptor affinity and interaction of new indole derivatives.
Farmaco (Società chimica italiana : 1989) 1993;48(2):285-95.
1993: Antonio Da Settimo; Giampaolo Primofiore; Federico Da Settimo; A Bianucci; Claudia Martini; G Senatore; Antonio Lucacchini
Synthesis and benzodiazepine receptor affinity of N-(indol-3-ylglyoxylyl)-dipeptide derivatives. Structural requirements for inverse agonist/antagonist receptor interactions.
Drug design and discovery 1993;10(3):199-211.
1992: Antonio Da Settimo; Giampaolo Primofiore; Federico Da Settimo; Anna Maria Marini
Synthesis and antiinflammatory properties of 2-aminobenzimidazole derivatives.
Farmaco (Società chimica italiana : 1989) 1992;47(10):1293-313.
1992: A M Bianucci; Antonio Da Settimo; Federico Da Settimo; Giampaolo Primofiore; Claudia Martini; Gino Giannaccini; Antonio Lucacchini
Benzodiazepine receptor affinity and interaction of some N-(indol-3-ylglyoxylyl)amine derivatives.
Journal of medicinal chemistry 1992;35(12):2214-20.
1990: Giampaolo Primofiore; Anna Maria Marini; Federico Da Settimo; C Salvadori; Claudia Martini; Antonio Lucacchini; Gino Giannaccini
Specific inhibition of benzodiazepine receptor binding by some N-(2-methyl or 1,2-dimethylindol-3-ylglyoxylyl)amino acid derivatives.
Farmaco (Società chimica italiana : 1989) 1990;45(3):341-51.
1989: Giampaolo Primofiore; Anna Maria Marini; Federico Da Settimo; Claudia Martini; A Bardellini; Gino Giannaccini; Antonio Lucacchini
Specific inhibition of benzodiazepine receptor binding by some N-(indol-3-ylglyoxylyl)amino acid derivatives: stereoselective interactions.
Journal of medicinal chemistry 1989;32(12):2514-8.
1989: P Caroti; C Ceccotti; Federico Da Settimo; Giampaolo Primofiore; J S Franzone; M C Reboani; Carlo Cravanzola
Synthesis, antilipidemic and platelet antiaggregatory activity of 2-aminobenzimidazole amide derivatives.
Farmaco (Società chimica italiana : 1989) 1989;44(3):227-55.