1430415-03-4Relevant articles and documents
A stereo configuration-activity study of 3-iodo-4-(2-methylcyclohexyloxy)-6-phenethylpyridin-2(2H)-ones as potency inhibitors of HIV-1 variants
Wu, Shaotong,Yin, Qianqian,Zhao, Liang,Fan, Ningning,Tang, Xiaowan,Zhao, Jianxiong,Sheng, Tao,Guo, Ying,Tian, Chao,Zhang, Zhili,Xu, Weisi,Liu, Zhenming,Jiang, Shibo,Ma, Liying,Liu, Junyi,Wang, Xiaowei
, p. 1413 - 1420 (2016/02/03)
3-Iodo-4-(2′-methylcyclohexyloxy)-6-phenethylpyridin-2(1H)-ones, as effective non-nucleoside reverse transcriptase inhibitors, were synthesized and resolved with different configurations. Biological results revealed that the trans-racemate 2b exhibited more potent activity than the cis-isomers. Noticeably, the trans-(S,S)-enantiomer 2e turned out to be significantly more potent than its counterpart enantiomer 2d against wild-type and double-mutant strains with high selectivity indexes.