کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1370671 | 981824 | 2011 | 4 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Acylglycinamides as inhibitors of glycine transporter type 1
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
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چکیده انگلیسی
A screening hit was used as the basis for the core structure of a new series of acylglycinamide GlyT-1 inhibitors. Investigation of the SAR around four areas of diversity used facile chemistry to prepare compounds quickly. By focussing on reducing the lipophilicity and improving the aqueous solubility in the series we were able to prepare a compound (17e) with a good level of activity at GlyT-1, selectivity over GlyT-2 and moderate oral bioavailability.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 21, Issue 20, 15 October 2011, Pages 6176–6179
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 21, Issue 20, 15 October 2011, Pages 6176–6179
نویسندگان
Richard Blunt, Roderick Porter, Amanda Johns, David Nash, Gemma Puckey, Paul Wyman, Hugh Herdon, Simon Teague, Victoria Hadden, Stefano Fontana, Laurie Gordon,