期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 19, 期 20, 页码 5864-5868出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.08.074
关键词
Soluble epoxide hydrolase; Nicotinamides; Epoxyeicosatrienoic acids; Inhibitors
A series of potent nicotinamide inhibitors of soluble epoxides hydrolase (sEH) is disclosed. This series was designed using structure-based deconstruction and a combination of two HTS hit series, resulting in hybrid analogs that retained the optimal potency from one series, and acceptable in vitro metabolic stability from the other. Structure-guided optimization of these analogs gave rise to nanomolar inhibitors of human sEH that had acceptable plasma exposure to qualify them as probes to determine the in vivo phenotypic consequences of sEH inhibition. (C) 2009 Elsevier Ltd. All rights reserved.
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