High affinity central benzodiazepine receptor ligands: Synthesis and structure-activity relationship studies of a new series of pyrazolo[4,3-c]quinolin-3-ones

被引：38

作者：

Savini, L

Massarelli, P

Nencini, C

Pellerano, C

Biggio, G

Maciocco, A

Tuligi, G

Carrieri, A

Cinone, N

Carotti, A

机构：

[1] Univ Bari, Dipartimento Farm Chim, I-70125 Bari, Italy

[2] Univ Siena, Dipartimento Farm Chim Tecnol, I-53100 Siena, Italy

[3] Univ Cagliari, Dipartimento Biol Sperimentale, I-09123 Cagliari, Italy

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 1998年 / 6卷 / 04期

关键词：

central benzodiazepine receptor ligands; pyrazolo[4,3-c]quinolin-3-ones; QSAR; S-35-TBPS binding; pharmacophore refinement;

D O I：

10.1016/S0968-0896(97)10039-6

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

A large series of 2-aryl(heteroaryl)-2,5-dihydropyrazolo[4,3-c]quinolin-3-(3H)-ones, carrying appropriate substituents at the quinoline and N-2-phenyl rings, were prepared and tested as central benzodiazepine receptor ligands. Results from structure-affinity relationship studies were in full agreement with previously proposed pharmacophore models and, in addition, quantitative structure-activity analysis gave further significant insight into the main molecular determinants of high benzodiazepine receptor affinity. The intrinsic activity of some active ligands was also determined and preliminary discussed. (C) 1998 Published by Elsevier Science Ltd. All rights reserved.

引用

页码：389 / 399

页数：11

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[1] SYNTHETIC AND COMPUTER-ASSISTED ANALYSES OF THE PHARMACOPHORE FOR THE BENZODIAZEPINE RECEPTOR INVERSE AGONIST SITE [J].