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

Hyunjin M Kim,Michelle D Smith,Jae-Hun Kim,Mary Ann Caplen,Tin Yau Chan,Brian A McKittrick,John A Cook,Margaret van Heek,Jean Lachowicz

Bioorganic & Medicinal Chemistry Letters（2013）

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摘要

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.

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关键词

DGAT1 inhibitors,Treatment for dyslipidemia,Scaffold hopping

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