Identification of 2-aminooxazole amides as acyl-CoA: Diacylglycerol acyltransferase 1 (DGAT1) inhibitors through scaffold hopping strategy
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- 作者：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
- 关键词：DGAT1 inhibitors ; Treatment for dyslipidemia ; Scaffold hopping
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：1 December, 2013
- 年：2013
- 卷：23
- 期：23
- 页码：6410-6414
- 全文大小：3132 K
文摘
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.