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Lead optimization of a pyridine-carboxamide series as DGAT-1 inhibitors |
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| Authors: | 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 |
| Institution: | 1. Department of Chemical Research, Merck Research Laboratories, 126 E. Lincoln Ave., Rahway, NJ 07065, USA;2. Department of Drug Metabolism, Merck Research Laboratories, 126 E. Lincoln Ave., Rahway, NJ 07065, USA;3. Department of Biological Research, Merck Research Laboratories, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA |
| Abstract: | 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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