Synthesis and structure-activity relationship of piperidine-derived non-urea soluble epoxide hydrolase inhibitors

Journal Article · Fri Sep 27 00:00:00 EDT 2013 · Bioorg. Med. Chem. Lett.

DOI:https://doi.org/10.1016/j.bmcl.2012.11.084· OSTI ID:1094867

Pecic, Stevan; Pakhomova, Svetlana; Newcomer, Marcia E.; Morisseau, Christophe; Hammock, Bruce D.; Zhu, Zhengxiang; Rinderspacher, Alison; Deng, Shi-Xian ^[1]

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1. UCD

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.

• Research Organization: Argonne National Lab. (ANL), Argonne, IL (United States). Advanced Photon Source (APS)
• Sponsoring Organization: OTHERNIH
• OSTI ID: 1094867
• Journal Information: Bioorg. Med. Chem. Lett., Vol. 23, Issue (2) ; 01, 2013; ISSN 0960-894X
• Country of Publication: United States
• Language: ENGLISH