کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1361439 | 981463 | 2008 | 6 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Synthesis and anticonvulsant evaluation of N-substituted isoquinoline AMPA receptor antagonists
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Synthesis and anticonvulsant evaluation of N-substituted isoquinoline AMPA receptor antagonists Synthesis and anticonvulsant evaluation of N-substituted isoquinoline AMPA receptor antagonists](/preview/png/1361439.png)
چکیده انگلیسی
In our previous studies a ligand-based approach led to the identification of noncompetitive AMPA receptor antagonists containing isoquinoline scaffold. In an attempt to perform a systematic SAR study, we synthesized new N-substituted-isoquinolines bearing the most salient features described by our 3D pharmacophore model. All compounds were screened against audiogenic seizures and some derivatives showed anticonvulsant properties. Compound 24, the most active of the series, was also tested in vitro using the patch–clamp technique and proved to antagonize AMPA-mediated effects.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 16, Issue 5, 1 March 2008, Pages 2379–2384
Journal: Bioorganic & Medicinal Chemistry - Volume 16, Issue 5, 1 March 2008, Pages 2379–2384
نویسندگان
Rosaria Gitto, Laura De Luca, Benedetta Pagano, Rita Citraro, Giovanbattista De Sarro, Lara Costa, Lucia Ciranna, Alba Chimirri,