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ACS Med Chem Lett. 2016 Oct 31;7(12):1156-1160. eCollection 2016 Dec 8.

Design, Conformation, and Crystallography of 2-Naphthyl Phenyl Ethers as Potent Anti-HIV Agents.

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Department of Chemistry, Yale University , New Haven, Connecticut 06520-8107, United States.
Department of Pharmacology, Yale University School of Medicine , New Haven, Connecticut 06520-8066, United States.


Catechol diethers that incorporate a 7-cyano-2-naphthyl substituent are reported as non-nucleoside inhibitors of HIV-1 reverse transcriptase (NNRTIs). Many of the compounds have 1-10 nM potencies toward wild-type HIV-1. An interesting conformational effect allows two unique conformers for the naphthyl group in complexes with HIV-RT. X-ray crystal structures for 4a and 4f illustrate the alternatives.


Anti-HIV agents; NNRTIs; protein crystallography

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