Abstract
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.
| Original language | English (US) |
|---|---|
| Pages (from-to) | 1259-1262 |
| Number of pages | 4 |
| Journal | ACS Medicinal Chemistry Letters |
| Volume | 5 |
| Issue number | 11 |
| DOIs | |
| State | Published - Nov 13 2014 |
Bibliographical note
Publisher Copyright:© 2014 American Chemical Society.
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This output contributes to the following UN Sustainable Development Goals (SDGs)
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SDG 3 Good Health and Well-being
Keywords
- Anti-HIV agents
- NNRTIs
- protein crystallography
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