Design, synthesis, and evaluation of diarylpyridines and diarylanilines as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.

Journal Article (Journal Article)

On the basis of the structures and activities of our previously identified non-nucleoside reverse transcriptase inhibitors (NNRTIs), we designed and synthesized two sets of derivatives, diarylpyridines (A) and diarylanilines (B), and tested their anti-HIV-1 activity against infection by HIV-1 NL4-3 and IIIB in TZM-bl and MT-2 cells, respectively. The results showed that most compounds exhibited potent anti-HIV-1 activity with low nanomolar EC50 values, and some of them, such as 13m, 14c, and 14e, displayed high potency with subnanomolar EC50 values, which were more potent than etravirine (TMC125, 1) in the same assays. Notably, these compounds were also highly effective against infection by multi-RTI-resistant strains, suggesting a high potential to further develop these compounds as a novel class of NNRTIs with improved antiviral efficacy and resistance profile.

Full Text

Duke Authors

Cited Authors

  • Tian, X; Qin, B; Wu, Z; Wang, X; Lu, H; Morris-Natschke, SL; Chen, CH; Jiang, S; Lee, K-H; Xie, L

Published Date

  • December 9, 2010

Published In

Volume / Issue

  • 53 / 23

Start / End Page

  • 8287 - 8297

PubMed ID

  • 21049929

Pubmed Central ID

  • PMC3050082

Electronic International Standard Serial Number (EISSN)

  • 1520-4804

Digital Object Identifier (DOI)

  • 10.1021/jm100738d


  • eng

Conference Location

  • United States