کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1376906 | 981967 | 2008 | 6 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
7-Azaindole derivatives as potential partial nicotinic agonists
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: 7-Azaindole derivatives as potential partial nicotinic agonists 7-Azaindole derivatives as potential partial nicotinic agonists](/preview/png/1376906.png)
چکیده انگلیسی
We have investigated a series of 7-azaindoles as potential partial agonists of the α4β2 nicotinic acetylcholine receptor (nAChR). Three series of 7-azaindole derivatives have been synthesized and evaluated for rat brain neuronal nicotinic receptor affinity and functional activity. Compound (+)-51 exhibited the most potent nAChR binding (Ki = 10 nM). Compound 30A demonstrated both moderate binding affinity and partial agonist potency, thus representing a promising lead for the indications of cognition and smoking cessation.
A series of 7-azaindoles was investigated as potential partial agonists of the α4β2 nicotinic acetylcholine receptor (nAChR).Figure optionsDownload as PowerPoint slide
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 18, Issue 1, 1 January 2008, Pages 188–193
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 18, Issue 1, 1 January 2008, Pages 188–193
نویسندگان
Axel R. Stoit, Arnold P. den Hartog, Harry Mons, Sjoerd van Schaik, Nynke Barkhuijsen, Cees Stroomer, Hein K.A.C. Coolen, Jan Hendrik Reinders, Tiny J.P. Adolfs, Martina van der Neut, Hiskias Keizer, Chris G. Kruse,