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The efficacy and cardiac evaluation of aminomethyl tetrahydronaphthalene ketopiperazines: a novel class of potent MCH-R1 antagonists |
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| Authors: | Méndez-Andino José L Colson Anny-Odile Meyers Kenneth M Mitchell Maria C Hodge Karen Howard Jeremy M Kim Nicholas Ackley David C Holbert Jerry K Mittelstadt Scott W Dowty Martin E Obringer Cindy M Suchanek Paula Reizes Ofer Hu X Eric Wos John A |
| Institution: | Procter & Gamble Pharmaceuticals, 8700 Mason-Montgomery Road, Mason, OH 45039, USA. mendezandino.jl@pg.com |
| Abstract: | The design, synthesis, and biological studies of a novel class of MCH-R1 antagonists based on an aminotetrahydronaphthalene ketopiperazine scaffold is described. Compounds within this class promoted significant body weight reduction in mouse diet induced obesity studies. The potential for hERG blockage activity and QT interval studies in anesthetized dogs are discussed. |
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