Synthesis and HIV-1 inhibition of novel benzimidazole derivatives

Bioorganic & Medicinal Chemistry Letters
1995.0

Abstract

A range of novel benzimidazole derivatives, some bearing analogy to TIBO, have been synthesized, and evaluated for inhibition of HIV-1 infectivity. The most active and selective compounds are a series of N-alkoxy-2-alkylbenzimidazoles, several having EC50 < 10~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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