SYNTHESIS AND ANTILIPOLYTIC ACTIVITIES OF QUINOLYL CARBANILATES AND RELATED ANALOGS
SYNTHESIS AND ANTILIPOLYTIC ACTIVITIES OF QUINOLYL CARBANILATES AND RELATED ANALOGS
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DOI：
10.1021/jm00384a011
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发表时间：
1987-01-01
影响因子：
7.3
通讯作者：
SUTHERLAND, CA
中科院分区：
文献类型：
--
作者：
MUSSER, JH;CHAKRABORTY, U;SUTHERLAND, CA
A series of quinolyl carbanilates was prepared and tested as antilipolytic agents. These compounds inhibited production of glycerol from rat adipocytes and inhibited liberation of free fatty acids from triolein by canine cardiac triglyceride lipases. An extensive structure-activity relationship study indicated that 8-quinolyl 4-methoxycarbanilate (1) contained features necessary for maximum potency in vitro. Substituting a benzofuranyl group for the quinolyl group of 1 provided the most interesting compound on the basis of both potency and structural novelty. 7-Benzofuranyl 4-methoxycarbanilate (44) has IC50''s of 16 and 0.3 .mu.M in the myocardial lipase and rat adipocyte assays, respectively. In vivo, compound 44 was orally active as an inhibitor (97% at 25 mg/kg) of lipolysis in the rat.
