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

Publication ,  Journal Article
Tian, X; Qin, B; Lu, H; Lai, W; Jiang, S; Lee, K-H; Chen, CH; Xie, L
Published in: Bioorg Med Chem Lett
September 15, 2009

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.

Duke Scholars

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Published In

Bioorg Med Chem Lett

DOI

EISSN

1464-3405

Publication Date

September 15, 2009

Volume

19

Issue

18

Start / End Page

5482 / 5485

Location

England

Related Subject Headings

  • Structure-Activity Relationship
  • Pyridines
  • Medicinal & Biomolecular Chemistry
  • Humans
  • HIV-1
  • HIV Reverse Transcriptase
  • HIV Infections
  • Drug Resistance, Viral
  • Anti-HIV Agents
  • 3405 Organic chemistry
 

Citation

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Tian, X., Qin, B., Lu, H., Lai, W., Jiang, S., Lee, K.-H., … Xie, L. (2009). Discovery of diarylpyridine derivatives as novel non-nucleoside HIV-1 reverse transcriptase inhibitors. Bioorg Med Chem Lett, 19(18), 5482–5485. https://doi.org/10.1016/j.bmcl.2009.07.080
Tian, Xingtao, Bingjie Qin, Hong Lu, Weihong Lai, Shibo Jiang, Kuo-Hsiung Lee, Chin Ho Chen, and Lan Xie. “Discovery of diarylpyridine derivatives as novel non-nucleoside HIV-1 reverse transcriptase inhibitors.Bioorg Med Chem Lett 19, no. 18 (September 15, 2009): 5482–85. https://doi.org/10.1016/j.bmcl.2009.07.080.
Tian X, Qin B, Lu H, Lai W, Jiang S, Lee K-H, et al. Discovery of diarylpyridine derivatives as novel non-nucleoside HIV-1 reverse transcriptase inhibitors. Bioorg Med Chem Lett. 2009 Sep 15;19(18):5482–5.
Tian, Xingtao, et al. “Discovery of diarylpyridine derivatives as novel non-nucleoside HIV-1 reverse transcriptase inhibitors.Bioorg Med Chem Lett, vol. 19, no. 18, Sept. 2009, pp. 5482–85. Pubmed, doi:10.1016/j.bmcl.2009.07.080.
Tian X, Qin B, Lu H, Lai W, Jiang S, Lee K-H, Chen CH, Xie L. Discovery of diarylpyridine derivatives as novel non-nucleoside HIV-1 reverse transcriptase inhibitors. Bioorg Med Chem Lett. 2009 Sep 15;19(18):5482–5485.
Journal cover image

Published In

Bioorg Med Chem Lett

DOI

EISSN

1464-3405

Publication Date

September 15, 2009

Volume

19

Issue

18

Start / End Page

5482 / 5485

Location

England

Related Subject Headings

  • Structure-Activity Relationship
  • Pyridines
  • Medicinal & Biomolecular Chemistry
  • Humans
  • HIV-1
  • HIV Reverse Transcriptase
  • HIV Infections
  • Drug Resistance, Viral
  • Anti-HIV Agents
  • 3405 Organic chemistry