کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1360211 | 981428 | 2009 | 8 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Development of 3-substituted-1H-indole derivatives as NR2B/NMDA receptor antagonists
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
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چکیده انگلیسی
A combined ligand-based and structure-based approach has previously allowed us to identify NR2B/NMDA receptor antagonists containing indole scaffold. In order to further explore the main structure activity relationships of this class of derivatives we herein report the design, synthesis and biological evaluation of new analogues. Some derivatives demonstrated to produce significant anticonvulsant properties and NMDA antagonism. The most active of them (3d) showed NR2B binding affinity equipotent to that of ifenprodil. These results were also corroborated by computational studies.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 17, Issue 4, 15 February 2009, Pages 1640–1647
Journal: Bioorganic & Medicinal Chemistry - Volume 17, Issue 4, 15 February 2009, Pages 1640–1647
نویسندگان
Rosaria Gitto, Laura De Luca, Stefania Ferro, Rita Citraro, Giovambattista De Sarro, Lara Costa, Lucia Ciranna, Alba Chimirri,