Discovery of orally active carboxylic acid derivatives of 2-phenyl-5-trifluoromethyloxazole-4-carboxamide as potent diacylglycerol acyltransferase-1 inhibitors for the potential treatment of obesity and diabetes

DOI: 10.1021/jm101580m

Source and publish data:

Journal of Medicinal Chemistry p. 2433 - 2446 (2011)

Update date:2022-08-05

Topics: Inhibitors Obesity Discovery Orally Active carboxylic acid derivatives diabetes

Authors:

Qian, Yimin

Wertheimer, Stanley J.

Ahmad, Mushtaq

Cheung, Adrian Wai-Hing

Firooznia, Fariborz

Hamilton, Matthew M.

Hayden, Stuart

Li, Shiming

Marcopulos, Nicholas

McDermott, Lee

Tan, Jenny

Yun, Weiya

Guo, Liang

Pamidimukkala, Anjula

Chen, Yingsi

Huang, Kuo-Sen

Ramsey, Gwendolyn B.

Whittard, Toni

Conde-Knape, Karin

Taub, Rebecca

Rondinone, Cristina M.

Tilley, Jefferson

Bolin, David

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Article abstract of DOI:10.1021/jm101580m

Diacylglycerol acyltransferase-1 (DGAT-1) is the enzyme that catalyzes the final and committed step of triglyceride formation, namely, the acylation of diacylglycerol with acyl coenzyme A. DGAT-1 deficient mice demonstrate resistance to weight gain on hig

Full text of DOI:10.1021/jm101580m

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Product name:4-{5-[(2-phenyl-5-trifluoromethyloxazole-4-carbonyl)amino]pyridin-2-yl}piperazine-1-carboxylic acid ethyl ester

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