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

文献索引：Bioorg. Med. Chem. Lett. 16(10) , 2748-52, (2006)

全文：HTML全文

摘要

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.