Winston Ho

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

Abstract 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.

C-19 functional steroids IX·1,2 further synthesis and biological evaluation of 2,19-disubtituted compounds

Abstract The synthesis of 2β, 19-epoxy-5a-pregnane-3,20-dione and the related 2,19 lactone is described. Bromination of these bridged A-ring steroids gives the corresponding 4a-bromo steroids, as shown by the n.m.r. spectra. The results of some biological tests on these and related compounds are presented; none of the tested compounds are active.