کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1378929 | 982014 | 2005 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Discovery of 4-(dimethylamino)quinazolines as potent and selective antagonists for the melanin-concentrating hormone receptor 1
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
A series of 4-(dimethylamino)quinazoline based antagonists of the melanin-concentrating hormone receptor 1 (MCH-R1) is described. This series was derived from a lead compound, AR129330, identified by HTS of a GPCR-directed library using a functional assay with a constitutively activated (CART) form of the receptor. The preliminary optimization resulted in the identification of compounds 20, 21, and 23.
High-throughput screening of our in-house GPCR-directed library uncovered a series of 4-(dimethylamino)quinazolines as melanin-concentrating hormone receptor 1 (MCH-R1) antagonists (e.g., AR129330). The synthesis and early SAR investigation of this series are reported.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 15, Issue 10, 16 May 2005, Pages 2565–2569
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 15, Issue 10, 16 May 2005, Pages 2565–2569
نویسندگان
Kosuke Kanuma, Katsunori Omodera, Mariko Nishiguchi, Takeo Funakoshi, Shigeyuki Chaki, Graeme Semple, Thuy-Anh Tran, Bryan Kramer, Debbie Hsu, Martin Casper, Bill Thomsen, Nigel Beeley, Yoshinori Sekiguchi,