کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1374458 981919 2009 5 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Synthesis and pharmacological evaluation of aminopyrimidine series of 5-HT1A partial agonists
کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Synthesis and pharmacological evaluation of aminopyrimidine series of 5-HT1A partial agonists
چکیده انگلیسی

Aminopyrimidine 2 (4-(1-(2-(1H-indol-3-yl)ethyl)piperidin-3-yl)-N-cyclopropylpyrimidin-2-amine) emerged from a high throughput screen as a novel 5-HT1A agonist. This compound showed moderate potency for 5-HT1A in binding and functional assays, as well as moderate metabolic stability. Implementation of a strategy for improving metabolic stability by lowering the lipophilicity (c Log D) led to identification of methyl ether 31 (4-(1-(2-(1H-indol-3-yl)ethyl)piperidin-3-yl)-N-(2-methoxyethyl)pyrimidin-2-amine) as a substantially improved compound within the series.

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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 19, Issue 4, 15 February 2009, Pages 1159–1163
نویسندگان
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