896085-17-9Relevant academic research and scientific papers
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)
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.
MMP-13 selective isonipecotamide α-sulfone hydroxamates
Kolodziej, Stephen A.,Hockerman, Susan L.,Decrescenzo, Gary A.,McDonald, Joseph J.,Mischke, Debbie A.,Munie, Grace E.,Fletcher, Theresa R.,Stehle, Nathan,Swearingen, Craig,Becker, Daniel P.
scheme or table, p. 3561 - 3564 (2010/10/01)
A series of N-aryl isonipecotamide α-sulfone hydroxamate derivatives has been prepared utilizing a combination of solution-phase and resin-bound library technologies to afford compounds that are potent and highly selective for MMP-13.
