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Pyrazole acids as niacin receptor agonists for the treatment of dyslipidemia |
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| Authors: | Darby Schmidt Abigail Smenton Subharekha Raghavan Ester Carballo-Jane Silvi Lubell Tanya Ciecko Tom G. Holt Michael Wolff Andrew Taggart Larissa Wilsie Mihajlo Krsmanovic Ning Ren Daniel Blom Kang Cheng Peggy E. McCann M. Gerard Waters James Tata Steven Colletti |
| Affiliation: | 1. Department of Medicinal Chemistry, Merck Research Laboratories, Merck & Co., Inc., Rahway, NJ 07065-0900, USA;2. Department of Cardiovascular Disease, Merck Research Laboratories, Merck & Co., Inc., Rahway, NJ 07065-0900, USA |
| Abstract: | Niacin is an effective drug for raising HDL cholesterol and reducing coronary risks, but patients show low compliance with treatment due to severe facial flushing upon taking the drug. A series of bicyclic pyrazole carboxylic acids were synthesized and tested for their ability to activate the niacin receptor. One analog, 23, showed improved potency and lacked flushing at doses that effectively altered the lipid profile of rats. |
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