کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1358722 | 981359 | 2015 | 7 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Discovery and structure-guided optimization of tert-butyl 6-(phenoxymethyl)-3-(trifluoromethyl)benzoates as liver X receptor agonists
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
To obtain potent liver X receptor (LXR) agonists, a structure–activity relationship study was performed on a series of tert-butyl benzoate analogs. As the crystal structure analysis suggested applicable interactions between the LXR ligand-binding domain and the ligands, two key functional groups were introduced. The introduction of the hydroxyl group on the C6-position of the benzoate part enhanced the agonistic activity in a cell-based assay, and the carboxyl group in terminal improved the pharmacokinetic profile in mice, respectively. The obtained compound 32b increased blood ABCA1 mRNA expression without plasma TG elevation in both mice and cynomolgus monkeys.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 25, Issue 18, 15 September 2015, Pages 3914–3920
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 25, Issue 18, 15 September 2015, Pages 3914–3920
نویسندگان
Yumi Matsui, Takahiro Yamaguchi, Takanori Yamazaki, Masayuki Yoshida, Masami Arai, Naoki Terasaka, Shoko Honzumi, Kenji Wakabayashi, Shinko Hayashi, Daisuke Nakai, Hiroyuki Hanzawa, Kazuhiko Tamaki,