Picomolar Inhibitors of HIV-1 Reverse Transcriptase: Design and Crystallography of Naphthyl Phenyl Ethers | Zendy

WonGil Lee | Zendy; Kathleen M. Frey | Zendy; Ricardo GallardoMacias | Zendy; Krasimir A. Spasov | Zendy; Mariela Bollini | Zendy; Karen S. Anderson | Zendy; William L. Jorgensen | Zendy

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Picomolar Inhibitors of HIV-1 Reverse Transcriptase: Design and Crystallography of Naphthyl Phenyl Ethers

Author(s) -

WonGil Lee,

Kathleen M. Frey,

Ricardo GallardoMacias,

Krasimir A. Spasov,

Mariela Bollini,

Karen S. Anderson,

William L. Jorgensen

Publication year - 2014

Publication title -

acs medicinal chemistry letters

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 1.065

H-Index - 66

ISSN - 1948-5875

DOI - 10.1021/ml5003713

Subject(s) - reverse transcriptase , substituent , nucleoside reverse transcriptase inhibitor , chemistry , human immunodeficiency virus (hiv) , stereochemistry , catechol , enzyme , virology , biology , rna , biochemistry , gene

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 Å resolution is also reported for the key compound 6e with HIV-RT.

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