|
|||||
|
|
Aminomethyl tetrahydronaphthalene ketopiperazine MCH-R1 antagonists--Increasing selectivity over hERG |
|
| Authors: | Meyers Kenneth M Méndez-Andino José L Colson Anny-Odile Warshakoon Namal C Wos John A Mitchell Maria C Hodge Karen M Howard Jeremy M Ackley David C Holbert Jerry K Mittelstadt Scott W Dowty Martin E Obringer Cindy M Reizes Ofer Hu X Eric |
| Institution: | Procter & Gamble Pharmaceuticals, 8700 Mason-Montgomery Road, Mason, OH 45039, USA. |
| Abstract: | A direct correlation between hERG binding and QTc prolongation was established for a series of aminomethyl tetrahydronaphthalene ketopiperazine MCH-R1 antagonists. Compounds within this class with greater selectivity over hERG were developed. Compound 4h proved to have the best profile, with MCH-R1 Ki = 16 nm and hERG IC50 = 25 microM. |
| Keywords: | |
| 本文献已被 ScienceDirect PubMed 等数据库收录！ | |