SYNTHESIS AND HIV-1 INHIBITION OF NOVEL BENZIMIDAZOLE DERIVATIVES

A range of novel benzimidazole derivatives, some bearing analogy to TI BO, have been synthesized, and evaluated for inhibition of HIV-I infec tivity. The most active and selective compounds are a series of N-alko xy-2-alkyl benzimidazoles, several having EC(50) < 10 mu M (one sub-mi cromolar at 600nM), and selectivity ratios of 10-167. The most selecti ve benzimidazoles, 18a, 18c, show modest RT inhibition, and binding as says indicate gp120-binding is not a target.