کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1371981 | 981863 | 2009 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Design and synthesis of piperazinylpyrimidinones as novel selective 5-HT2C agonists
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
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چکیده انگلیسی
This Letter reports the design and synthesis of several novel series of piperazinyl pyrimidinones as 5-HT2C agonists. Several of the compounds presented exhibit good in vitro potency and selectivity over the closely related 5-HT2A and 5-HT2B receptors. Compound 11 was active in in vivo models of stress urinary incontinence.
The design, synthesis and biological activity of several novel series of piperazinyl pyrimidinones is described. Compound 11 showed efficacy in a pre-clinical model of urethral function which highlights potential efficacy in stress urinary incontinence.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 19, Issue 18, 15 September 2009, Pages 5346–5350
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 19, Issue 18, 15 September 2009, Pages 5346–5350
نویسندگان
Mark D. Andrews, Martin P. Green, Charlotte M.N. Allerton, David V. Batchelor, Julian Blagg, Alan D. Brown, David W. Gordon, Gordon McMurray, Daniel J. Millns, Carly L. Nichols, Lesa Watson,