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Bioorg Med Chem Lett. 2013 Dec 1;23(23):6410-4. doi: 10.1016/j.bmcl.2013.09.048. Epub 2013 Sep 25.

Identification of 2-aminooxazole amides as acyl-CoA: diacylglycerol acyltransferase 1 (DGAT1) inhibitors through scaffold hopping strategy.

Author information

1
Discovery Chemistry, Merck Research Laboratories, 2000 Galloping Hill Road, Kenilworth, NJ 07033, USA. Electronic address: hyunjin.kim@merck.com.

Abstract

A scaffold hopping strategy was successfully applied in discovering 2-aminooxazole amides as potent DGAT1 inhibitors for the treatment of dyslipidemia. Further optimization in potency and PK properties resulted in a lead series with oral in vivo efficacy in a mouse postprandial triglyceridemia (PPTG) assay.

KEYWORDS:

DGAT1 inhibitors; Scaffold hopping; Treatment for dyslipidemia

PMID:
24120540
DOI:
10.1016/j.bmcl.2013.09.048
[Indexed for MEDLINE]
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