- 6,7-Dihydro-5H-cyclopenta[d]pyrazolo[1,5-a]pyrimidines and their derivatives as novel corticotropin-releasing factor 1 receptor antagonists.
6,7-Dihydro-5H-cyclopenta[d]pyrazolo[1,5-a]pyrimidines and their derivatives as novel corticotropin-releasing factor 1 receptor antagonists.
Bioorganic & medicinal chemistry (2011-08-26)
Tetsuji Saito, Tetsuo Obitsu, Takashi Kondo, Toshiaki Matsui, Yuuki Nagao, Kensuke Kusumi, Naoya Matsumura, Sonoko Ueno, Akihiro Kishi, Seishi Katsumata, Yoshifumi Kagamiishi, Hisao Nakai, Masaaki Toda
PMID21865047
RÉSUMÉ
To identify an orally active corticotropin-releasing factor 1 receptor antagonist, a series of 6,7-dihydro-5H-cyclopenta[d]pyrazolo[1,5-a]pyrimidines and their derivatives were designed, synthesized and evaluated. An in vitro study followed by in vivo and pharmacokinetic studies of these heterotricyclic compounds led us to the discovery of an orally active CRF1 receptor antagonist. The results of a structure-activity relationship study are presented.
MATÉRIAUX