Synthesis and anti-HIV activities of urea-pETT analogs belonging to a new class of potent non-nucleoside HIV-1 Reverse transcriptase inhibitors

A series of potent specific HIV-1 RT inhibitory compounds is described. The compounds are urea analogs of PETT ( henyl thyl hiazole hiourea) derivatives and the series includes derivatives with an ethyl linker (1–6) and conformationally restricted analogs (7–13). The antiviral activity is determined both at the RT level and in cell culture on both native and mutant forms of HIV-1. Many compounds display activity in the nM range against wt-RT.