کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1366972 | 981611 | 2007 | 4 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
5-HT2C antagonists based on fused heterotricyclic templates: Design, synthesis and biological evaluation
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: 5-HT2C antagonists based on fused heterotricyclic templates: Design, synthesis and biological evaluation 5-HT2C antagonists based on fused heterotricyclic templates: Design, synthesis and biological evaluation](/preview/png/1366972.png)
چکیده انگلیسی
Design, synthesis and properties of a new tricyclic series of selective 5-HT2C receptor antagonists are reported. Conformational analysis of a 2-phenyl-dihydropyrrolone scaffold suggested that ring fusion, locking coplanarity between the rings of this moiety, might be tolerated by the 5-HT2C receptor. An interesting effect of this is the change of the nature of the carbon–carbon double bond of the lactam ring from vinylic to aromatic. The changes were found to result in a favourable profile at both, receptor and in vivo level.
Design, synthesis and properties of a new tricyclic series of selective 5-HT2C receptor antagonists are reported.Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 17, Issue 2, 15 January 2007, Pages 424–427
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 17, Issue 2, 15 January 2007, Pages 424–427
نویسندگان
Dieter Hamprecht, Fabrizio Micheli, Giovanna Tedesco, Daniele Donati, Marcella Petrone, Silvia Terreni, Martyn Wood,