6, 7-Dihydro-5H-cyclopenta [d] pyrazolo [1, 5-a] pyrimidines and their derivatives as novel corticotropin-releasing factor 1 receptor antagonists

…, T Matsui, Y Nagao, K Kusumi, N Matsumura…

Index: Saito, Tetsuji; Obitsu, Tetsuo; Kondo, Takashi; Matsui, Toshiaki; Nagao, Yuuki; Kusumi, Kensuke; Matsumura, Naoya; Ueno, Sonoko; Kishi, Akihiro; Katsumata, Seishi; Kagamiishi, Yoshifumi; Nakai, Hisao; Toda, Masaaki Bioorganic and Medicinal Chemistry, 2011 , vol. 19, # 18 p. 5432 - 5445

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Citation Number: 12

Abstract

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 ...