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Get Free AccessCatechol diethers that incorporate a 6-cyano-1-naphthyl substituent have been explored as non-nucleoside inhibitors of HIV-1 reverse transcriptase (NNRTIs). Promising compounds are reported that show midpicomolar activity against the wild-type virus and sub-20 nM activity against viral variants bearing Tyr181Cys and Lys103Asn mutations in HIV-RT. An X-ray crystal structure at 2.49 Å resolution is also reported for the key compound 6e with HIV-RT.
Won‐Gil Lee, Kathleen M. Frey, Ricardo Gallardo‐Macias, Krasimir A. Spasov, Mariela Bollini, Karen S. Anderson, William L. Jorgensen (2014). Picomolar Inhibitors of HIV-1 Reverse Transcriptase: Design and Crystallography of Naphthyl Phenyl Ethers. ACS Medicinal Chemistry Letters, 5(11), pp. 1259-1262, DOI: 10.1021/ml5003713.
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Type
Article
Year
2014
Authors
7
Datasets
0
Total Files
0
Language
English
Journal
ACS Medicinal Chemistry Letters
DOI
10.1021/ml5003713
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