- Design, synthesis, and structure-activity relationships of a series of 2-Ar-8-methyl-5-alkylaminoquinolines as novel CRF1 receptor antagonists
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We designed and synthesized a series of 2-Ar-8-methyl-5- alkylaminolquinolines as potent corticotropin-releasing factor 1 (CRF 1) receptor antagonists. The structure-activity relationships of substituents at each position (R3, R5, R 5′, and R8) was investigated. By derivatization, three compounds (6, 14b, and 14c) were identified as orally active CRF 1 receptor antagonists.
- Takeda, Kunitoshi,Terauchi, Taro,Hashizume, Minako,Shin, Kogyoku,Ino, Mitsuhiro,Shibata, Hisashi,Yonaga, Masahiro
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p. 5372 - 5378
(2012/09/22)
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