Structural features of a new class of non nucleoside HIV-1 RT inhibitors

The crystal structures of a new pharmacologicai class of HIV-1 inhibitors are reported. Of a large series of thiazolobenzimidazoles the TBZ (1-(2’,6’difluorophenyl)-1H, 3H-thiazolo[3,4-a] benzimidazole {NSC 625487} is a highly potent inhibitor of human immunodeficiency virus-induced cell killing and viral replication in a variety of human cell lines at concentrations not cytotoxic to the host cells. All the compounds assume a butterfiylike conformation that appears particulariy important in RT inhibitors