Synthesis, SAR study, and biological evaluation of a series of piperazine ureas as fatty acid amide hydrolase (FAAH) inhibitors

…, T Matsumoto, T Kawamura, A Nishimura…

文献索引：Kono, Mitsunori; Matsumoto, Takahiro; Kawamura, Toru; Nishimura, Atsushi; Kiyota, Yoshihiro; Oki, Hideyuki; Miyazaki, Junichi; Igaki, Shigeru; Behnke, Craig A.; Shimojo, Masato; Kori, Masakuni Bioorganic and Medicinal Chemistry, 2013 , vol. 21, # 1 p. 28 - 41

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被引用次数: 16

摘要

A series of piperazine ureas was designed, synthesized, and evaluated for their potential as novel orally available fatty acid amide hydrolase (FAAH) inhibitors that are therapeutically effective against pain. We carried out an optimization study of the lead compound 3 to improve its DMPK profile as well as in vitro potency. We identified the thiazole compound 60j with potent inhibitory activity, high brain permeability, and good bioavailability. Compound ...