کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10586868 | 981409 | 2012 | 20 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Synthesis and structure-activity relationships of 8-substituted-2-aryl-5-alkylaminoquinolines: Potent, orally active corticotropin-releasing factor-1 receptor antagonists
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
We previously reported a series of 8-methyl-2-aryl-5-alkylaminoquinolines as a novel class of corticotropin-releasing factor-1 (CRF1) receptor antagonists. A critical issue encountered for this series of compounds was low aqueous solubility at physiological pH (pH 7.4). To address this issue, derivatization at key sites (R2, R3, R5, R5â², and R8) was performed and the relationships between structure and solubility were examined. As a result, it was revealed that introduction of a methoxy substituent at the C8 position had a positive impact on the solubility of the derivatives. Consequently, through in vivo and in vitro biological studies, compound 21d was identified as a potent, orally active CRF1 receptor antagonist with improved physicochemical properties.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 20, Issue 22, 15 November 2012, Pages 6559-6578
Journal: Bioorganic & Medicinal Chemistry - Volume 20, Issue 22, 15 November 2012, Pages 6559-6578
نویسندگان
Kunitoshi Takeda, Taro Terauchi, Minako Hashizume, Kohdoh Shikata, Ryota Taguchi, Kaoru Murata-Tai, Masae Fujisawa, Yoshinori Takahashi, Kogyoku Shin, Mitsuhiro Ino, Hisashi Shibata, Masahiro Yonaga,