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Titolo:
High affinity central benzodiazepine receptor ligands. Part 2: Quantitative structure-activity relationships and comparative molecular field analysisof pyrazolo[4,3-c]quinolin-3-ones
Autore:
Savini, L; Chiasserini, L; Pellerano, C; Biggio, G; Maciocco, E; Serra, M; Cinone, N; Carrieri, A; Altomare, C; Carotti, A;
Indirizzi:
Univ Bari, Dipartimento Farm Chim, I-70125 Bari, Italy Univ Bari Bari Italy I-70125 Dipartimento Farm Chim, I-70125 Bari, Italy Univ Siena, Dipartimento Farm Chim Tecnol, I-53100 Siena, Italy Univ Siena Siena Italy I-53100 to Farm Chim Tecnol, I-53100 Siena, Italy Univ Cagliari, Dipartimento Biol Sperimentale, I-09123 Cagliari, Italy Univ Cagliari Cagliari Italy I-09123 erimentale, I-09123 Cagliari, Italy Univ G DAnnunzio, Dipartimento Sci Farm, I-66013 Chieti Scalo, CH, Italy Univ G DAnnunzio Chieti Scalo CH Italy I-66013 13 Chieti Scalo, CH, Italy
Titolo Testata:
BIOORGANIC & MEDICINAL CHEMISTRY
fascicolo: 2, volume: 9, anno: 2001,
pagine: 431 - 444
SICI:
0968-0896(200102)9:2<431:HACBRL>2.0.ZU;2-O
Fonte:
ISI
Lingua:
ENG
Soggetto:
CHIRAL STATIONARY-PHASE; IMIDAZOLINE RECEPTOR; RELATIONSHIP MODELS; INVERSE AGONIST; BINDING; LIPOPHILICITY; ANALOGS; PHARMACOPHORE; SUBSTITUENT; INHIBITION;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
70
Recensione:
Indirizzi per estratti:
Indirizzo: Carotti, A Univ Bari, Dipartimento Farm Chim, Via E Orabona 4, I-70125 Bari, Italy Univ Bari Via E Orabona 4 Bari Italy I-70125 70125 Bari, Italy
Citazione:
L. Savini et al., "High affinity central benzodiazepine receptor ligands. Part 2: Quantitative structure-activity relationships and comparative molecular field analysisof pyrazolo[4,3-c]quinolin-3-ones", BIO MED CH, 9(2), 2001, pp. 431-444

Abstract

A large series of 2-aryl(heteroaryl)-2,5-dihydropyrazolo[4,3-c]quinolin-3(3H)-ones (PQ, 106 compounds), carrying appropriate substituents at the quinoline and N-2-phenyl rings, were designed, prepared and tested as central benzodiazepine receptor ligands. Compounds with an affinity significantly higher than the parent compound CGS-8216 were obtained, the most active ligand showing a pIC(50) = 10.35. Hansch and comparative molecular field analyses gave coherent results suggesting the main structural requirements of highreceptor binding affinity. The possible formation of a three-centred hydrogen bond (HB) at the HB donor site H-2, as a key interaction for high receptor binding affinity, was assessed by the calculation and comparison of themolecular electrostatic potentials of a series of selected ligands. (C) 2001 Elsevier Science Ltd. All rights reserved.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 02/04/20 alle ore 22:25:45