کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1369869 981791 2016 7 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Synthesis, structure–activity relationships, and biological evaluation of a series of benzamides as potential multireceptor antipsychotics
ترجمه فارسی عنوان
سنتز، ارتباطات فعالیت ساختاری و ارزیابی بیولوژیکی مجموعه ای از بنزامید ها به عنوان آنتی سایکوتیک های بالقوه چندتایی
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
چکیده انگلیسی

In the present study, a series of benzamides, endowed with potent dopamine D2, serotonin 5-HT1A and 5-HT2A receptors properties, was synthesized and evaluated as potential antipsychotics. Among them, 3-(4-(4-(6-fluorobenzo[d]isoxazol-3-yl)-piperidin-1-yl)butoxy)-N-methylbenzamide (21) and its fluoro-substituted analogue (22) held the best pharmacological binding profiles. They not only presented potent activities for D2, 5-HT1A, and 5-HT2A receptors, but were also endowed with low activities for 5-HT2C, H1 receptors and hERG channels, suggesting a low propensity of inducing weight gain and QT prolongation. In animal models, compounds 21 and 22 reduced phencyclidine-induced hyperactivity with a high threshold for catalepsy induction. It thus provides potential candidates for further preclinical studies.

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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 26, Issue 13, 1 July 2016, Pages 3141–3147
نویسندگان
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