Design, synthesis, and biological evaluation of novel piperidine-4-carboxamide derivatives as potent CCR5 inhibitors

S Hu, Q Gu, Z Wang, Z Weng, Y Cai, X Dong…

文献索引：Hu, Suwen; Gu, Quan; Wang, Zhilong; Weng, Zhiyong; Cai, Yunrui; Dong, Xiaowu; Hu, Yongzhou; Liu, Tao; Xie, Xin European Journal of Medicinal Chemistry, 2014 , vol. 71, p. 259 - 266

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被引用次数: 6

摘要

Abstract Based on a putative 'Y shape'pharmacophore model of CCR5 inhibitors, a series of novel piperidine-4-carboxamide derivatives were designed and synthesized using a group- reverse strategy. Among synthesized target compounds, 16g (IC 50= 25.73 nM) and 16i (IC 50= 25.53 nM) showed equivalent inhibitory activity against CCR5 to that of the positive control maraviroc (IC 50= 25.43 nM) in calcium mobilization assay. Selected compounds ...