期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 19, 期 19, 页码 5716-5721出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.08.006
关键词
Amide mimics; Aminoheterocycles; Inhibitors; sEH; Soluble epoxide hydrolase
Distinct from previously reported urea and amide inhibitors of soluble epoxide hydrolase (sEH), a novel class of inhibitors were rationally designed based on the X-ray structure of this enzyme and known amide inhibitors. The structure-activity relationship (SAR) study was focused on improving the sEH inhibitory activity. Aminobenzisoxazoles emerged to be the optimal series, of which a potent human sEH inhibitor 7t was identified with a good pharmacokinetics (PK) profile. The strategy of employing aminoheterocycles as amide replacements may represent a general approach to develop mimics of known hydrolase or protease inhibitors containing an amide moiety. (C) 2009 Elsevier Ltd. All rights reserved.
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