Diacylglycerol O-acyltransferase, also known as diglyceride acyltransferase(DGAt), is key enzyme in triglyceride synthesis. DGAT1 catalyzes  final and rate-limiting step in the triacylglycerol synthesis from 1,2-diacylglycerol(DAG) and long chain fatty acyl CoA as substrates. Thus, DGAT plays an essential role in the metabolism of cellular diacylglycerol and is critically important for triglyceride production and energy storage homostasis. Herein we report the design and development of several series of bicyclic carboxylic acid derivatives as potent and selective DGAT1 inhibitor. In vivo mouse postprandial triglyceridemia atudies have shown these DGAT1 inhibitors ruduce plasma triglyceride level significantly following a lipid challenge.

Design and synthesis of potent and selective acyl-CoA:diacylglycerol acyltransferaseI (DGAT1) inhibitor:novel indole and benzomorpholine derivatives

244th National Meeting (2012)

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