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The discovery of high affinity agonists of GPR109a with reduced serum shift and improved ADME properties |
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| Authors: | Imbriglio Jason E DiRocco Daniel Bodner Rena Raghavan Subharekha Chen Weichun Marley Daria Esser Craig Holt Tom G Wolff Michael S Taggart Andrew K P Waters M Gerard Tata James R Colletti Steven L |
| Institution: | a Department of Medicinal Chemistry, Merck Research Laboratories, Merck & Co., Inc., PO Box 2000, Rahway, NJ 07065-0900, USA b Department of Drug Metabolism, Merck Research Laboratories, Merck & Co., Inc., PO Box 2000, Rahway, NJ 07065-0900, USA c Department of Cardiovascular Diseases, Merck Research Laboratories, Merck & Co., Inc., PO Box 2000, Rahway, NJ 07065-0900, USA |
| Abstract: | Amino-anthranilic acid derivatives have been identified as a new class of low serum shifted, high affinity full agonists of the human orphan G-protein-coupled receptor GPR109a with improved ADME properties. |
| Keywords: | Niacin Atherosclerosis Anthranilic acid |
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