Challenges in the development of mGluR5 positive allosteric modulators: the discovery of CPPHA |
| |
| Authors: | Zhao Zhijian Wisnoski David D O'Brien Julie A Lemaire Wei Williams David L Jacobson Marlene A Wittman Marion Ha Sookhee N Schaffhauser Herve Sur Cyrille Pettibone Doug J Duggan Mark E Conn P Jeffrey Hartman George D Lindsley Craig W |
| |
| Institution: | Department of Medicinal Chemistry, Merck & Co., Inc., PO Box 4, West Point, PA 19486, USA. zhijian_zhao@merck.com |
| |
| Abstract: | This Letter describes, for the first time, the synthesis and SAR, developed through an iterative analog library approach, that led to the discovery of the positive allosteric modulator (PAM) of the metabotropic glutamate receptor mGluR5 CPPHA. Binding to a unique allosteric binding site distinct from other mGluR5 PAMs, CPPHA has been the focus of numerous pharmacology studies by several laboratories. |
| |
| Keywords: | |
| 本文献已被 ScienceDirect PubMed 等数据库收录！ |
|
