Tetrazole thioacetanilides: Potent non-nucleoside inhibitors of WT HIV reverse transcriptase and its K103N mutant

A series of aryltetrazolylacetanilides was synthesized and evaluated as HIV-1 non-nucleoside reverse transcriptase inhibitors on wild-type virus and on the clinically relevant K103N mutant strain. Extensive SAR investigation led to potent compounds, with nanomolar activity on K103N, and orally bioavailable in rats.

Graphical abstractSAR study on tetrazole thioacetanilides as NNRTIs led to potent compounds, with nanomolar activity on both WT HIV and on the clinically relevant K103N mutant, submicromolar activity in infected cells and orally bioavailable in rats.Figure optionsDownload full-size imageDownload as PowerPoint slide