Synthesis and anti-HIV activity of 2-naphthyl substituted DAPY analogues as non-nucleoside reverse transcriptase inhibitors

Nine newly 6-cynao-2-naphthyl substituted diarylpyrimidines (DAPY) were synthesized as non-nucleoside reverse transcriptase inhibitors on the basis of our previous work. The antiviral and cytotoxicity evaluation indicated that these compounds displayed strong activity against wild-type HIV-1 at nanomolar concentrations with selectivity index SI greater than 23 779. The most active compounds 3c and 3e exhibited activity against the double mutant (103N+181C) strains at an EC50 of 0.16 and 0.15 μM, and were more activity than that of efavirenz.

Nine newly 6-cyano-2-naphthyl substituted DAPY analogues were synthesized and evaluated as inhibitors of the HIV-1 wild-type and double mutant (K103N+Y181C) strains in this paper.Figure optionsDownload as PowerPoint slide