کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1376316 | 981954 | 2007 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
The synthesis and structure–activity relationship studies of selective acetyl-CoA carboxylase inhibitors containing 4-(thiazol-5-yl)but-3-yn-2-amino motif: Polar region modifications
دانلود مقاله + سفارش ترجمه
دانلود مقاله ISI انگلیسی
رایگان برای ایرانیان
کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
The structure–activity relationship study focused on the polar region of the HTS hit A-80040 (1) producing several series of potent and selective ACC2 inhibitors. The SAR suggests a compact lipophilic pocket that does not tolerate polar and ionic groups. Replacement of the hydroxyurea group with isoxazoles improves ACC2 selectivity while maintaining potency. Variations at the propargylic site of 11a reduce ACC2 potency.
Potent and selective ACC2 inhibitors were synthesized by modifying the polar region of a HTS hit and the SAR suggests a compact and lipophilic binding pocket.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 17, Issue 6, 15 March 2007, Pages 1803–1807
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 17, Issue 6, 15 March 2007, Pages 1803–1807
نویسندگان
Xiangdong Xu, Moshe Weitzberg, Robert F. Keyes, Qun Li, Rongqi Wang, Xiaojun Wang, Xiaolin Zhang, Ernst U. Frevert, Heidi S. Camp, Bruce A. Beutel, Hing L. Sham, Yu Gui Gu,