Bioorganic & Medicinal Chemistry Letters 2006-05-15

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

Ester Muraglia, Olaf D Kinzel, Ralph Laufer, Michael D Miller, Gregory Moyer, Vandna Munshi, Federica Orvieto, Maria Cecilia Palumbi, Giovanna Pescatore, Michael Rowley, Peter D Williams, Vincenzo Summa

Index: Bioorg. Med. Chem. Lett. 16(10) , 2748-52, (2006)

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Abstract

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.