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Tetrazole thioacetanilides: potent non-nucleoside inhibitors of WT HIV reverse transcriptase and its K103N mutant. 2006
Ester Muraglia, and
Olaf D Kinzel, and
Ralph Laufer, and
Michael D Miller, and
Gregory Moyer, and
Vandna Munshi, and
Federica Orvieto, and
Maria Cecilia Palumbi, and
Giovanna Pescatore, and
Michael Rowley, and
Peter D Williams, and
Vincenzo Summa
Department of Medicinal Chemistry, IRBM/MRL Rome, Via Pontina Km 30,600, 00040 Pomezia, Rome, Italy. Ester_Muraglia@merck.com
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.
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