کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1370132 | 981809 | 2011 | 4 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Discovery of 4-aminomethylphenylacetic acids as γ-secretase modulators via a scaffold design approach
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Discovery of 4-aminomethylphenylacetic acids as γ-secretase modulators via a scaffold design approach Discovery of 4-aminomethylphenylacetic acids as γ-secretase modulators via a scaffold design approach](/preview/png/1370132.png)
چکیده انگلیسی
Starting from literature examples of nonsteroidal anti-inflammatory drugs (NSAIDs)-type carboxylic acid γ-secretase modulators (GSMs) and using a scaffold design approach, we identified 4-aminomethylphenylacetic acid 4 with a desirable γ-secretase modulation profile. Scaffold optimization led to the discovery of a novel chemical series, represented by 6b, having improved brain penetration. Further SAR studies provided analog 6q that exhibited a good pharmacological profile. Oral administration of 6q significantly reduced brain Aβ42 levels in mice and rats.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 21, Issue 24, 15 December 2011, Pages 7277–7280
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 21, Issue 24, 15 December 2011, Pages 7277–7280
نویسندگان
Zhili Xin, Hairuo Peng, Andrew Zhang, Tina Talreja, Gnanasambandam Kumaravel, Lin Xu, Ellen Rohde, Mi-yong Jung, Melanie N. Shackett, David Kocisko, Sowmya Chollate, Anthone W. Dunah, Pamela A. Snodgrass-Belt, H. Moore Arnold, Arthur G. Taveras,