Discovery of 6-chloro-2-trifluoromethyl-7-aryl-7H-imidazo[1,2-a]imidazol-3-ylmethylamines, a novel class of corticotropin-releasing factor receptor type 1 (CRF1R) antagonists.
A novel series of [6-chloro-2-trifluoromethyl-7-aryl-7H-imidazo[1,2-a]imidazol-3-ylmethyl]-dialkylamines was discovered as potent CRF(1)R antagonists. The optimization of binding affinity in the series by the parallel reaction approach is discussed herein.
Zuev
Dmitry
D
Bristol-Myers Squibb Pharmaceutical Research Institute, Wallingford, CT 06492, USA. dmitry.zuev@bms.com
Vrudhula
Vivekananda M
VM
Michne
Jodi A
JA
Dasgupta
Bireshwar
B
Pin
Sokhom S
SS
Huang
Xiaohua Stella
XS
Wu
Dedong
D
Gao
Qi
Q
Zhang
Jie
J
Taber
Matthew T
MT
Macor
John E
JE
Dubowchik
Gene M
GM
D006801:Humans; D007093:Imidazoles / Q000737:chemistry* / Q000494:pharmacology; D008744:Methylamines / Q000737:chemistry* / Q000494:pharmacology; D011485:Protein Binding; D018019:Receptors, Corticotropin-Releasing Hormone / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship; D000099052:CRF Receptor, Type 1
D007093:Imidazoles; D008744:Methylamines; D018019:Receptors, Corticotropin-Releasing Hormone; D000099052:CRF Receptor, Type 1