| Literature DB >> 19645482 |
Hong C Shen1, Fa-Xiang Ding, Siyi Wang, Qiaolin Deng, Xiaoping Zhang, Yuli Chen, Gaochao Zhou, Suoyu Xu, Hsuan-Shen Chen, Xinchun Tong, Vincent Tong, Kaushik Mitra, Sanjeev Kumar, Christine Tsai, Andra S Stevenson, Lee-Yuh Pai, Magdalena Alonso-Galicia, Xiaoli Chen, Stephen M Soisson, Sophie Roy, Bei Zhang, James R Tata, Joel P Berger, Steven L Colletti.
Abstract
4-Substituted piperidine-derived trisubstituted ureas are reported as highly potent and selective inhibitors for sEH. The SAR outlines approaches to improve activity against sEH and reduce ion channel and CYP liability. With minimal off-target activity and a good PK profile, the benchmark 2d exhibited remarkable in vitro and ex vivo target engagement. The eutomer entA-2d also elicited vasodilation effect in rat mesenteric artery.Entities:
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Year: 2009 PMID： 19645482 DOI： 10.1021/jm900725r
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446