Discovery of N-(1-Ethylpropyl)-[3-methoxy-5-(2-methoxy-4-trifluoromethoxyphenyl)-6-methyl-pyrazin-2-yl] amine 59 (NGD 98− 2): An Orally Active Corticotropin …

…, SD Lombaert, R Brodbeck, M Gulianello…

Index: Hodgetts, Kevin J.; Ge, Ping; Yoon, Taeyoung; Lombaert, Stephane De; Brodbeck, Robbin; Gulianello, Michael; Kieltyka, Andrzej; Horvath, Raymond F.; Kehne, John H.; Krause, James E.; Maynard, George D.; Hoffman, Diane; Lee, Younglim; Fung, Laurence; Doller, Dario Journal of Medicinal Chemistry, 2011 , vol. 54, # 12 p. 4187 - 4206

Full Text: HTML

Citation Number: 8

Abstract

The design, synthesis, and structure− activity relationships of a novel series of pyrazines, acting as corticotropin releasing factor-1 (CRF-1) receptor antagonists, are described. Synthetic methodologies were developed to prepare a number of substituted pyrazine cores utilizing regioselective halogenation and chemoselective derivatization. Noteworthy, an efficient 5-step synthesis was developed for the lead compound 59 (NGD 98− 2), which ...

Related Articles:

More Articles...