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

被引：8
|
作者：
Kim, Hyunjin M. [1 ]
Smith, Michelle D. [2 ]
Kim, Jae-Hun [1 ]
Caplen, Mary Ann [1 ]
Chan, Tin Yau [1 ]
McKittrick, Brian A. [1 ]
Cook, John A. [2 ]
Van Heek, Margaret [2 ]
Lachowicz, Jean [2 ]
机构：
[1] Merck Res Labs, Discovery Chem, Kenilworth, NJ 07033 USA
[2] Merck Res Labs, Discovery Biol, Kenilworth, NJ 07033 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2013年 / 23卷 / 23期
关键词：
DGAT1; inhibitors; Treatment for dyslipidemia; Scaffold hopping; INSULIN-RESISTANCE; DISCOVERY; POTENT; OBESITY; MICE; PERMEABILITY; OPTIMIZATION; DERIVATIVES; MECHANISMS;
D O I：
10.1016/j.bmcl.2013.09.048
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
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. (C) 2013 Elsevier Ltd. All rights reserved.
引用
收藏
页码：6410 / 6414
页数：5
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