期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 30, 期 20, 页码 -出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2020.127463
关键词
FAAH; Inhibitors; Endocannabinoid; Covalent inhibitor; Anandamide; Serine hydrolase; Enzyme; Aryl urea
A series of mechanism-based heteroaryl urea fatty acid amide hydrolase (FAAH) inhibitors with fused bicyclic diamine cores is described. In contrast to compounds built around a piperazine core, most of the fused bicyclic diamine bearing analogs prepared exhibited greater potency against rFAAH than the human enzyme. Several compounds equipotent against both species were identified and profiled in vivo.
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