Bioorganic & Medicinal Chemistry 2011-09-15

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

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

文献索引：Bioorg. Med. Chem. 19(18) , 5432-45, (2011)

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摘要

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.Copyright © 2011 Elsevier Ltd. All rights reserved.