881833-22-3Relevant articles and documents
Design, synthesis, and biological evaluation of novel piperidine-4- carboxamide derivatives as potent CCR5 inhibitors
Hu, Suwen,Gu, Quan,Wang, Zhilong,Weng, Zhiyong,Cai, Yunrui,Dong, Xiaowu,Hu, Yongzhou,Liu, Tao,Xie, Xin
, p. 259 - 266 (2014/01/06)
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 (IC50 = 25.73 nM) and 16i (IC50 = 25.53 nM) showed equivalent inhibitory activity against CCR5 to that of the positive control maraviroc (IC50 = 25.43 nM) in calcium mobilization assay. Selected compounds were further tested for their antiviral activity in HIV-1 single cycle assay. Two compounds, 16g and 16i, displayed antiviral activity with IC 50 values of 73.01 nM and 94.10 nM, respectively. Additionally, the pharmacokinetic properties and inhibitory potency against hERG of 16g were evaluated, providing a foundation for ongoing optimization.
N-sulfonylpiperidine cannabinoid receptor 1 antagonists
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Page/Page column 12, (2008/06/13)
The present application describes compounds according to Formula I, wherein R1, R2, R3, R4, X and Y are described herein. Additionally, the present application describes pharmaceutical compositions comprising at least one compound according to Formula I and optionally one or more additional therapeutic agents. Finally, the present application describes methods of treatment using the compounds according to Formula I both alone and in combination with one or more additional therapeutic agents.