BICYCLIC IMIDAZO DERIVATIVES, A NEW CLASS OF HIGHLY SELECTIVE INHIBITORS FOR THE HUMAN-IMMUNODEFICIENCY-VIRUS TYPE-1

In the search for new antiviral agents against human immunodeficiency virus, different members of two imidazoheterocycle families (imidazoth iazoles, imidazopyridines) have been found to display potent inhibitor y effects on the replication of HIV-1. Three of these derivatives, whi ch show significant anti-HIV-1 activity, have been chosen for further studies. The analysis of these compounds and their comparison to AZT a nd TIBO revealed that these bicyclic imidazo derivatives represent a c lass of highly specific inhibitors of HIV-1, but not of HIV-2 or simia n immunodeficiency virus (SIV). Their inhibition of HIV-1 is mediated through interaction with the reverse transcriptase (RT). The mechanism of action of these bicyclic imidazo derivatives may be similar to tha t of the other non-nucleoside RT inhibitors (NNRTIs).