Potential anxiolytic agents .2. Improvement of oral efficacy for the pyrido[1,2-a]benzimidazole (PBI) class of GABA-A receptor modulators

被引：37

作者：

Maryanoff, BE

McComsey, DF

Ho, W

Shank, RP

Dubinsky, B

机构：

[1] Drug Discovery, R. W. Johnson Pharmaceutical Research Institute, Spring House

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1996年 / 6卷 / 03期

关键词：

D O I：

10.1016/0960-894X(96)00025-X

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

We have further explored the structure-activity relationships of pyrido[1,2-a]benzimidazole (PBI) derivatives (viz. prototype 1), a novel series of central GABA-A receptor modulators, with the intent of enhancing oral efficacy. A study involving the introduction of acidic or basic groups led to the identification of RWJ-38293 (3a) as a potential anxiolytic agent.

引用

页码：333 / 338

页数：6

共 23 条

[1]

CHILDRESS SJ, 1981, BURGERS MED CHEM 3, P981

[2] NEW DEVICE FOR RAPID MEASUREMENT OF IMPAIRED MOTOR FUNCTION IN MICE [J].