2. Academic Validation
  3. Discovery of diarylpyridine derivatives as novel non-nucleoside HIV-1 reverse transcriptase inhibitors

Discovery of diarylpyridine derivatives as novel non-nucleoside HIV-1 reverse transcriptase inhibitors

  • Bioorg Med Chem Lett. 2009 Sep 15;19(18):5482-5. doi: 10.1016/j.bmcl.2009.07.080.
Xingtao Tian 1,  Bingjie Qin,  Hong Lu,  Weihong Lai,  Shibo Jiang,  Kuo-Hsiung Lee,  Chin Ho Chen,  Lan Xie
Affiliations

Affiliation

  • 1 Beijing Institute of Pharmacology and Toxicology, 27 Tai-Ping Road, Beijing 100850, China.
PMID: 19666220 DOI: 10.1016/j.bmcl.2009.07.080
Abstract

Two series (4 and 5) of diarylpyridine derivatives were designed, synthesized, and evaluated for anti-HIV-1 activity. The most promising compound, 5e, inhibited HIV-1 IIIB, NL4-3, and RTMDR1 with low nanomolar EC50 values and selectivity indexes of >10,000. The results of this study indicate that diarylpyridine can be used as a novel scaffold to derive a new class of potent NNRTIs, active against both wild-type and drug-resistant HIV-1 strains.

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