Jm. Gardiner et al., SYNTHESIS AND HIV-1 INHIBITION OF NOVEL BENZIMIDAZOLE DERIVATIVES, Bioorganic & medicinal chemistry letters, 5(12), 1995, pp. 1251-1254
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.