新型喹啉羧酸系列作为二酰甘油酰基转移酶1（DGAT1）抑制剂的发现。
Discovery of novel quinoline carboxylic acid series as DGAT1 inhibitors.
作者信息
Zhou Gang, Ting Pauline C, Wishart Grant, Zorn Nicolas, Aslanian Robert G, Lin Mingxiang, Smith Michelle, Walker Scott S, Cook John, Van Heek Margaret, Lachowicz Jean
机构信息
Department of Chemical Research, Merck Research Laboratories, 126 E. Lincoln Ave., Rahway, NJ 07065, USA.
Department of Chemical Research, Merck Research Laboratories, 126 E. Lincoln Ave., Rahway, NJ 07065, USA.
出版信息
Bioorg Med Chem Lett. 2014 Apr 1;24(7):1790-4. doi: 10.1016/j.bmcl.2014.02.028. Epub 2014 Feb 19.
Herein we report the design and synthesis of a series of novel bicyclic DGAT1 inhibitors with a carboxylic acid moiety. The optimization of the initial lead compound 7 based on in vitro and in vivo activity led to the discovery of potent indoline and quinoline classes of DGAT1 inhibitors. The structure-activity relationship studies of these novel series of bicyclic carboxylic acid derivatives as DGAT1 inhibitors are described.
在此，我们报告了一系列带有羧酸部分的新型双环DGAT1抑制剂的设计与合成。基于体外和体内活性对初始先导化合物7进行优化，从而发现了强效的吲哚啉类和喹啉类DGAT1抑制剂。本文描述了这些新型双环羧酸衍生物作为DGAT1抑制剂的构效关系研究。
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