کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
1362108 981478 2007 11 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Novel piperazines: Potent melanocortin-4 receptor antagonists with anxiolytic-like activity
موضوعات مرتبط
مهندسی و علوم پایه شیمی شیمی آلی
پیش نمایش صفحه اول مقاله
Novel piperazines: Potent melanocortin-4 receptor antagonists with anxiolytic-like activity
چکیده انگلیسی

In the present study, we found that a novel piperazine compound, 11a, showed a moderate affinity (IC50 = 333 nM) for the MC4 receptor. We developed the new type of piperazine compounds and found that mono-piperazine 11b exhibited a high-affinity (IC50 = 40.3 nM) for the MC4 receptor. We also found that a series of biphenyl analogues exhibited a high-affinity for the receptor, and in particular, compound 11j exhibited the highest affinity for the MC4 receptor with an IC50 value of 14.5 nM. Furthermore, some of these compounds, when administered orally, significantly reversed the stress-induced anxiety-like behavior in rats. In this paper, we report the synthesis, structure-activity relationships, and oral activity of the novel mono-piperazines as MC4 receptor antagonists.

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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 15, Issue 6, 15 March 2007, Pages 2375–2385
نویسندگان
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