Discovery of novel benzimidazolones as potent non-nucleoside reverse transcriptase inhibitors active against wild-type and mutant HIV-1 strains.

Molecular modeling studies led to the rational discovery of N(1)-arylsulfonyl-1,3-dihydro-2H-benzimidazol-2-one as a novel template for the design of new non-nucleoside reverse transcriptase inhibitors (NNRTIs) that are active against wild-type and mutant strains of HIV-1. It is worth noting that compound 3 proved to have antiretroviral activity similar to that of efavirenz and greater than that of nevirapine, two of the three NNRTIs currently available in antiretroviral therapy.