Design, synthesis, and biological evaluation of a series of piperazine ureas as fatty acid amide hydrolase inhibitors

M Kono, T Matsumoto, T Imaeda, T Kawamura…

文献索引：Kono, Mitsunori; Matsumoto, Takahiro; Imaeda, Toshihiro; Kawamura, Toru; Fujimoto, Shinji; Kosugi, Yohei; Odani, Tomoyuki; Shimizu, Yuji; Matsui, Hideki; Shimojo, Masato; Kori, Masakuni Bioorganic and Medicinal Chemistry, 2014 , vol. 22, # 4 p. 1468 - 1478

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被引用次数: 8

摘要

Abstract A series of piperazine ureas were designed, synthesized, and evaluated for their potential as novel orally efficacious fatty acid amide hydrolase (FAAH) inhibitors for the treatment of neuropathic and inflammatory pain. We carried out an optimization study of compound 5 to improve its in vitro FAAH inhibitory activity, and identified the 2- pyrimidinylpiperazine derivative 21d with potent inhibitory activity, favorable DMPK profile ...