Structural highlights
Publication Abstract from PubMed
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.
Synthesis and structure-activity relationship of piperidine-derived non-urea soluble epoxide hydrolase inhibitors.,Pecic S, Pakhomova S, Newcomer ME, Morisseau C, Hammock BD, Zhu Z, Rinderspacher A, Deng SX Bioorg Med Chem Lett. 2013 Jan 15;23(2):417-21. doi: 10.1016/j.bmcl.2012.11.084. , Epub 2012 Dec 1. PMID:23237835[1]
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.
References
- ↑ Pecic S, Pakhomova S, Newcomer ME, Morisseau C, Hammock BD, Zhu Z, Rinderspacher A, Deng SX. Synthesis and structure-activity relationship of piperidine-derived non-urea soluble epoxide hydrolase inhibitors. Bioorg Med Chem Lett. 2013 Jan 15;23(2):417-21. doi: 10.1016/j.bmcl.2012.11.084. , Epub 2012 Dec 1. PMID:23237835 doi:http://dx.doi.org/10.1016/j.bmcl.2012.11.084
