2. Academic Validation
  3. 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

  • Bioorg Med Chem. 2011 Sep 15;19(18):5432-45. doi: 10.1016/j.bmc.2011.07.055.
Tetsuji Saito 1,  Tetsuo Obitsu,  Takashi Kondo,  Toshiaki Matsui,  Yuuki Nagao,  Kensuke Kusumi,  Naoya Matsumura,  Sonoko Ueno,  Akihiro Kishi,  Seishi Katsumata,  Yoshifumi Kagamiishi,  Hisao Nakai,  Masaaki Toda
Affiliations

Affiliation

  • 1 Minase Research Institute, Ono Pharmaceutical Co., Ltd, 3-1-1 Sakurai, Shimamoto, Mishima, Osaka 618-8585, Japan. te.saitou@ono.co.jp
PMID: 21865047 DOI: 10.1016/j.bmc.2011.07.055
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 study are presented.

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