Synthesis and antilipolytic activities of quinolyl carbanilates and related analogs
作者:John H. Musser、Utpal Chakraborty、Kevin Bailey、Stan Sciortino、Carol Whyzmuzis、Dilip Amin、Charles A. Sutherland
DOI:10.1021/jm00384a011
日期:1987.1
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
制备了一系列喹啉基氨基甲酸酯并作为抗脂解剂进行了测试。这些化合物抑制犬心脏甘油三酸酯脂肪酶从大鼠脂肪细胞中产生甘油,并抑制游离脂肪酸从三油精中释放。广泛的构效关系研究表明,4-喹啉基4-甲氧基氨基甲酸酯(1)具有体外最大效价所必需的功能。基于效力和结构新颖性,用苯并呋喃基取代1的喹啉基提供了最有趣的化合物。7-Benzofuranyl 4-methoxycarbanilate(44)在心肌脂肪酶和大鼠脂肪细胞分析中的IC50分别为16和0.3 microM。在体内,化合物44在大鼠中作为口服脂解抑制剂(25%/ kg,97%)具有口服活性。