Design, Synthesis, and Structure–Activity Relationships of Novel Pyrazolo [5, 1-b] thiazole Derivatives as Potent and Orally Active Corticotropin-Releasing Factor 1 …

…, K Murata-Tai, M Fujisawa, K Shikata…

文献索引：Takahashi, Yoshinori; Hashizume, Minako; Shin, Kogyoku; Terauchi, Taro; Takeda, Kunitoshi; Yonaga, Masahiro; Shikata, Kodo; Taguchi, Ryota; Ino, Mitsuhiro; Shibata, Hisashi; Murata-Tai, Kaoru; Fujisawa, Masae; Hibi, Shigeki Journal of Medicinal Chemistry, 2012 , vol. 55, # 19 p. 8450 - 8463,14

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被引用次数: 5

摘要

This paper describes the design, synthesis, and structure–activity relationships of a novel series of 7-dialkylamino-3-phenyl-6-methoxy pyrazolo [5, 1-b] thiazole derivatives for use as selective antagonists of the corticotropin-releasing factor 1 (CRF1) receptor. The most promising compound, N-butyl-3-[4-(ethoxymethyl)-2, 6-dimethoxyphenyl]-6-methoxy-N- (tetrahydro-2 H-pyran-4-yl) pyrazolo [5, 1-b][1, 3] thiazole-7-amine (6t), showed high ...