SYNTHESIS AND ANTI-HIV ACTIVITIES OF UREA-PETT ANALOGS BELONGING TO ANEW CLASS OF POTENT NONNUCLEOSIDE HIV-1 REVERSE-TRANSCRIPTASE INHIBITORS

A series of potent specific HIV-1 RT inhibitory compounds is described . The compounds are urea analogs of PETT (PhenylEthylThiazoleThiourea) derivatives and the series includes derivatives with an ethyl linker (1-6) and conformationally restricted analogs (7-13). The antiviral ac tivity 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 th e nM range against wt-RT. (C) 1998 Elsevier Science Ltd. All rights re served.