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Bioorg Med Chem Lett. 2010 Jun 15;20(12):3703-7. doi: 10.1016/j.bmcl.2010.04.078. Epub 2010 Apr 22.

Rapid synthesis of an array of trisubstituted urea-based soluble epoxide hydrolase inhibitors facilitated by a novel solid-phase method.

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  • 1Department of Medicinal Chemistry, Boehringer Ingelheim Pharmaceuticals, Inc., Ridgefield, CT 06877, USA. jennifer.kowalski@boehringer-ingelheim.com

Abstract

A 270-membered library of trisubstituted ureas was synthesized and evaluated for inhibition of soluble epoxide hydrolase. Library design and reagent selection was guided by the use of a pharmacophore model and synthesis of the array was enabled with a general solid-phase method. This array approach facilitated multi-dimensional SAR around this series and identified functionality responsible for binding affinity, as well as opportunities for modulating the overall in vitro profiles of this class of soluble epoxide hydrolase inhibitors.

Copyright 2010 Elsevier Ltd. All rights reserved.

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