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Bioorg Med Chem Lett. 2010 Nov 15;20(22):6366-9. doi: 10.1016/j.bmcl.2010.09.094. Epub 2010 Sep 19.

2-Aryl benzimidazoles: human SCD1-specific stearoyl coenzyme-A desaturase inhibitors.

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1
Merck Frosst Centre for Therapeutic Research, 16711 Trans Canada Highway, Kirkland, Québec, Canada H9H 3L1. david_powell2@merck.com

Abstract

A series of potent, benzimidazole-based SCD inhibitors which demonstrate selectivity for the hSCD1 enzyme over the hSCD5 isoform are described. The compounds possess suitable cellular activity and pharmacokinetic properties which render them capable of inhibiting liver SCD activity in a mouse pharmacodynamic assay. These 2-aryl benzimidazoles may serve as valuable tools for studying selective hSCD1-inhibition.

PMID:
20933412
DOI:
10.1016/j.bmcl.2010.09.094
[Indexed for MEDLINE]
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