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

A series of novel S-DACO derivatives were designed by structure-based linker optimization strategy. Most compounds showed potential activities against HIV-1 with IC50 values ranging from 7.55 μmol/L to 0.018 μmol/L. Preliminary SAR and molecular modeling of these novel congeners were investigated. [...

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Veröffentlicht in:Chinese chemical letters 2021-03, Vol.32 (3), p.1020-1024
Hauptverfasser: 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
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Sprache:eng
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