Back to Search Start Over

2-Arylaminothiazoles as high-affinity corticotropin-Releasing factor 1 receptor (CRF1R) antagonists: synthesis, binding studies and behavioral efficacy

Authors :
Dubowchik, Gene M.
Michne, Jodi A.
Zuev, Dmitry
Schwartz, Wendy
Scola, Paul M.
James, Clint A.
Ruediger, Edward H.
Pin, Sokhom S.
Burris, Kevin D.
Balanda, Lynn A.
Gao, Qi
Wu, Dedong
Fung, Lawrence
Fiedler, Tracey
Browman, Kaitlin E.
Taber, Matthew T.
Zhang, Jie
Source :
Bioorganic & Medicinal Chemistry Letters. Nov2003, Vol. 13 Issue 22, p3997. 4p.
Publication Year :
2003

Abstract

2-Arylamino-4-trifluoromethyl-5-aminomethylthiazoles represent a novel series of high-affinity corticotropin releasing factor-1 receptor (CRF1R) antagonists that are prepared in three steps in good overall yields. Herein, we report binding SAR as well as anxiolytic activity of an exemplary compound (7a, Ki=8.6 nM) in a mouse canopy model. [Copyright &y& Elsevier]

Details

Language :
English
ISSN :
0960894X
Volume :
13
Issue :
22
Database :
Academic Search Index
Journal :
Bioorganic & Medicinal Chemistry Letters
Publication Type :
Academic Journal
Accession number :
11173380
Full Text :
https://doi.org/10.1016/j.bmcl.2003.08.055