SYNTHESIS AND HIV-1 INHIBITION OF NOVEL BENZIMIDAZOLE DERIVATIVES

被引：40

作者：

GARDINER, JM ^{[1
]}

LOYNS, CR ^{[1
]}

BURKE, A ^{[1
]}

KHAN, A ^{[1
]}

MAHMOOD, N ^{[1
]}

机构：

[1] MRC,CTR COLLABORAT,LONDON NW7 1AD,ENGLAND

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1995年 / 5卷 / 12期

关键词：

D O I：

10.1016/0960-894X(95)00203-6

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A range of novel benzimidazole derivatives, some bearing analogy to TIBO, have been synthesized, and evaluated for inhibition of HIV-I infectivity. The most active and selective compounds are a series of N-alkoxy-2-alkyl benzimidazoles, several having EC(50) < 10 mu M (one sub-micromolar at 600nM), and selectivity ratios of 10-167. The most selective benzimidazoles, 18a, 18c, show modest RT inhibition, and binding assays indicate gp120-binding is not a target.

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页码：1251 / 1254

页数：4

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