Synthesis and biological evaluation of isoxazole, oxazole, and oxadiazole containing heteroaryl analogs of biaryl ureas as DGAT1 inhibitors

…, L Doshi, N Potdar, AA Enose, RA Vishwakarma…

文献索引：Jadhav, Ravindra D.; Kadam, Kishorkumar S.; Kandre, Shivaji; Guha, Tandra; Reddy, M. Mahesh Kumar; Brahma, Manoja K.; Deshmukh, Nitin J.; Dixit, Amol; Doshi, Lalit; Potdar, Nisha; Enose, Arno A.; Vishwakarma, Ram A.; Sivaramakrishnan; Srinivasan, Shaila; Nemmani, Kumar V.S.; Gupte, Amol; Gangopadhyay, Ashok K.; Sharma, Rajiv European Journal of Medicinal Chemistry, 2012 , vol. 54, p. 324 - 342

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被引用次数: 22

摘要

Diacylglycerol acyltransferase, DGAT1, is a promising target enzyme for obesity due to its involvement in the committed step of triglyceride biosynthesis. Amino biphenyl carboxylic acids, exemplified by compound 4, are known potent inhibitors of hDGAT1. However the high cLogP and poor solubility of these biphenyl analogs might tend to limit their development. We have synthesized and evaluated compounds containing 3- ...