Lead optimization of a pyridine-carboxamide series as DGAT-1 inhibitors.

Pauline C Ting,Joe F Lee,Nicolas Zorn,Hyunjin M Kim,Robert G Aslanian,Mingxiang Lin,Michelle Smith,Scott S Walker,John Cook,Margaret Van Heek,Jean Lachowicz

Bioorganic & Medicinal Chemistry Letters（2013）

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摘要

The structure–activity relationship studies of a novel series of carboxylic acid derivatives of pyridine-carboxamides as DGAT-1 inhibitors is described. The optimization of the initial lead compound 6 based on in vitro and in vivo activity led to the discovery of key compounds 10j and 17h.

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关键词

DGAT-1 inhibitor,Inhibition of triacylglycerol synthesis,Treatment for obesity and diabetes

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