Picomolar Inhibitors of HIV-1 Reverse Transcriptase: Design and Crystallography of Naphthyl Phenyl Ethers
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- 作者：Won-Gil Lee ; Kathleen M. Frey ; Ricardo Gallardo-Macias ; Krasimir A. Spasov ; Mariela Bollini ; Karen S. Anderson ; William L. Jorgensen
- 刊名：ACS Medicinal Chemistry Letters
- 出版年：2014
- 出版时间：November 13, 2014
- 年：2014
- 卷：5
- 期：11
- 页码：1259-1262
- 全文大小：257K
- ISSN：1948-5875
文摘
Catechol 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 脜 resolution is also reported for the key compound 6e with HIV-RT.