Exploration of pyridine containing heteroaryl analogs of biaryl ureas as DGAT1 inhibitors

…, A Dixit, L Doshi, A Gupte, AK Gangopadhyay…

Index: Motiwala, Hashim; Kandre, Shivaji; Birar, Vishal; Kadam, Kishorkumar S.; Rodge, Atish; Jadhav, Ravindra D.; Mahesh Kumar Reddy; Brahma, Manoja K.; Deshmukh, Nitin J.; Dixit, Amol; Doshi, Lalit; Gupte, Amol; Gangopadhyay, Ashok K.; Vishwakarma, Ram A.; Srinivasan, Shaila; Sharma, Mamta; Nemmani, Kumar V.S.; Sharma, Rajiv Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 19 p. 5812 - 5817

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Citation Number: 11

Abstract

The diacylglycerol acyltransferase enzyme, DGAT1, presents itself as a potential target for obesity as this enzyme is dedicated to the final committed step in triglyceride biosynthesis. Biphenyl ureas, exemplified by compound 4, have been reported to be potent hDGAT1 inhibitors. We have synthesized and evaluated 2-pyridyl and 3-pyridyl containing biaryl ureas as hDGAT1 inhibitors. Our aim was to incorporate a heteroaryl scaffold within these ...