Optimization of 2,4-diarylanilines as non-nucleoside HIV-1 reverse transcriptase inhibitors.

Journal Article (Journal Article)

The current optimization of 2,4-diarylaniline analogs (DAANs) on the central phenyl ring provided a series of new active DAAN derivatives 9a-9e, indicating an accessible modification approach that could improve anti-HIV potency against wild-type and resistant strains, aqueous solubility, and metabolic stability. A new compound 9e not only exhibited extremely high potency against wild-type virus (EC(50) 0.53 nM) and several resistant viral strains (EC(50) 0.36-3.9 nM), but also showed desirable aqueous solubility and metabolic stability, which were comparable or better than those of the anti-HIV-1 drug TMC278 (2). Thus, new compound 9e might be a potential drug candidate for further development of novel next-generation NNRTIs.

Full Text

Duke Authors

Cited Authors

  • Sun, L-Q; Qin, B; Huang, L; Qian, K; Chen, C-H; Lee, K-H; Xie, L

Published Date

  • April 1, 2012

Published In

Volume / Issue

  • 22 / 7

Start / End Page

  • 2376 - 2379

PubMed ID

  • 22406117

Pubmed Central ID

  • PMC3309038

Electronic International Standard Serial Number (EISSN)

  • 1464-3405

Digital Object Identifier (DOI)

  • 10.1016/j.bmcl.2012.02.055


  • eng

Conference Location

  • England