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

Journal Article (Journal Article)

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.

Full Text

Duke Authors

Cited Authors

  • Tian, X; Qin, B; Lu, H; Lai, W; Jiang, S; Lee, K-H; Chen, CH; Xie, L

Published Date

  • September 15, 2009

Published In

Volume / Issue

  • 19 / 18

Start / End Page

  • 5482 - 5485

PubMed ID

  • 19666220

Pubmed Central ID

  • PMC2770631

Electronic International Standard Serial Number (EISSN)

  • 1464-3405

Digital Object Identifier (DOI)

  • 10.1016/j.bmcl.2009.07.080


  • eng

Conference Location

  • England