作为 DGAT-1 抑制剂的吡啶甲酰胺系列的先导优化。
Lead optimization of a pyridine-carboxamide series as DGAT-1 inhibitors.
机构信息
Department of Chemical Research, Merck Research Laboratories, 126 E. Lincoln Ave., Rahway, NJ 07065, USA.
出版信息
Bioorg Med Chem Lett. 2013 Feb 15;23(4):985-8. doi: 10.1016/j.bmcl.2012.12.040. Epub 2012 Dec 21.
PMID:23317570
Abstract
The structure-activity relationship studies of a novel series of carboxylic acid derivatives of pyridine-carboxamides as DGAT-1 inhibitors is described. The optimization of the initial lead compound 6 based on in vitro and in vivo activity led to the discovery of key compounds 10j and 17h.
摘要
本文描述了一系列新型吡啶甲酰胺羧酸衍生物作为 DGAT-1 抑制剂的构效关系研究。基于体外和体内活性对初始先导化合物 6 进行优化，发现了关键化合物 10j 和 17h。
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