Design, synthesis, and structure-activity relationships of a series of 2-Ar-8-methyl-5-alkylaminoquinolines as novel CRF(1) receptor antagonists |
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| Authors: | Kunitoshi Takeda Taro Terauchi Minako Hashizume Kogyoku Shin Mitsuhiro Ino Hisashi Shibata Masahiro Yonaga |
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| Institution: | Medicinal Chemistry, Tsukuba Research Laboratories, Eisai Co., Ltd, 5-1-3 Tokodai, Tsukuba-shi, Ibaraki 300-2635, Japan. |
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| Abstract: | 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 (R(3), R(5), R(5'), and R(8)) was investigated. By derivatization, three compounds (6, 14b, and 14c) were identified as orally active CRF(1) receptor antagonists. |
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| Keywords: | Corticotropin-releasing factor Depression Pharmacophore Structure–activity relationships Stress |
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