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J Med Chem. 2009 Aug 27;52(16):5009-12. doi: 10.1021/jm900725r.

Discovery of a highly potent, selective, and bioavailable soluble epoxide hydrolase inhibitor with excellent ex vivo target engagement.

Author information

1
Merck Research Laboratories, Merck & Co., Inc., Rahway, NJ 07065-0900, USA. hong_shen@merck.com

Abstract

4-Substituted piperidine-derived trisubstituted ureas are reported as highly potent and selective inhibitors for sEH. The SAR outlines approaches to improve activity against sEH and reduce ion channel and CYP liability. With minimal off-target activity and a good PK profile, the benchmark 2d exhibited remarkable in vitro and ex vivo target engagement. The eutomer entA-2d also elicited vasodilation effect in rat mesenteric artery.

PMID:
19645482
DOI:
10.1021/jm900725r
[Indexed for MEDLINE]

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