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Structure-based linker optimization of 6-(2-cyclohexyl-1-alkyl)-2-(2-oxo-2-phenylethylsulfanyl)pyrimidin-4(3H)-ones as potent non-nucleoside HIV-1 reverse transcriptase inhibitors

Authors :
Li, Daxiong
Zhang, Chunsheng
Ding, Wei
Huang, Siming
Yu, Le
Lu, Nan
Pan, Wenkai
Li, Yiming
De Clercq, Erik
Pannecouque, Christophe
Zhang, Hongbing
Wang, Yueping
He, Yanping
Chen, Fener
Source :
Chinese Chemical Letters; March 2021, Vol. 32 Issue: 3 p1020-1024, 5p
Publication Year :
2021

Abstract

A series of novel S-DACO derivatives were designed by structure-based linker optimization strategy. Most compounds showed potential activities against HIV-1 with IC50values ranging from 7.55 μmol/L to 0.018 μmol/L. Preliminary SAR and molecular modeling of these novel congeners were investigated.

Details

Language :
English
ISSN :
10018417
Volume :
32
Issue :
3
Database :
Supplemental Index
Journal :
Chinese Chemical Letters
Publication Type :
Periodical
Accession number :
ejs54331332
Full Text :
https://doi.org/10.1016/j.cclet.2020.09.035