期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 20, 期 20, 页码 6030-6033出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.08.066
关键词
DGAT1 inhibitors; Pyrrolopyridazines; DGAT1; Acyl CoA: diacylglycerol acyltransferase
new structural class of DGAT1 inhibitors was discovered and the structure-activity relationship was explored. The pyrrolotriazine core of the original lead molecule was changed to a pyrrolopyridazine core providing an increase in potency. Further exploration resulted in optimization of the propyl group at C7 and the discovery that the ester at C6 could be replaced by five-membered heterocyclic rings. The analogs prepared have DGAT1 IC(50) values ranging from >10 mu M to 48 nM. (c) 2010 Elsevier Ltd. All rights reserved.
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