کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10585513 | 981367 | 2012 | 6 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Synthesis and biological evaluation of benzoisothiazole derivatives possessing N,N-dimethylformimidamide group as 5-HT6 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 biological evaluation of benzoisothiazole derivatives possessing N,N-dimethylformimidamide group as 5-HT6 receptor antagonists Synthesis and biological evaluation of benzoisothiazole derivatives possessing N,N-dimethylformimidamide group as 5-HT6 receptor antagonists](/preview/png/10585513.png)
چکیده انگلیسی
A series of novel N,N-dimethyl-Nâ²-(5-(Ar-sulfonamido) benzo[d]isothiazol-3-yl)formimidamides was designed and synthesized as 5-HT6 ligands. Here N,N-dimethyl formimidamides was used as a replacement for an aminoethyl moiety. In vitro functional assays demonstrated compounds 9b and 9i significantly inhibited the 5-HT-induced Ca2+ increases (9b; IC50 = 0.36 μM and 9i; IC50 = 0.44 μM), indicating that 9b and 9i were potent 5-HT6 receptor antagonists. Compounds 9i also showed good selectivity on the 5-HT6 over 5-HT4 and 5-HT7 receptors.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 20, Issue 8, 15 April 2012, Pages 2707-2712
Journal: Bioorganic & Medicinal Chemistry - Volume 20, Issue 8, 15 April 2012, Pages 2707-2712
نویسندگان
Euna Yoo, Faisal Hayat, Hyewhon Rhim, Hea-Young Park Choo,