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
Language
- eng
Conference Location
- England