期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 23, 期 2, 页码 417-421出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2012.11.084
关键词
Soluble epoxide hydrolase; Non-urea inhibitors; Hypertension; Human liver microsomes stability
资金
- NIEHS [R01 ES002710]
- NIH [R01 HL 107887]
- Louisiana Governors' Biotechnology Initiative
- National Center for Research Resources from the National Institutes of Health [5P41RR015301-10]
- National Institute of General Medical Sciences from the National Institutes of Health [8 P41 GM103403-10]
- U.S. DOE [DE-AC02-06CH11357]
A series of potent amide non-urea inhibitors of soluble epoxide hydrolase (sEH) is disclosed. The inhibition of soluble epoxide hydrolase leads to elevated levels of epoxyeicosatrienoic acids (EETs), and thus inhibitors of sEH represent one of a novel approach to the development of vasodilatory and anti-inflammatory drugs. Structure-activities studies guided optimization of a lead compound, identified through high-throughput screening, gave rise to sub-nanomolar inhibitors of human sEH with stability in human liver microsomal assay suitable for preclinical development. Published by Elsevier Ltd.
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