کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10583872 | 981312 | 2013 | 27 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Design and bio-evaluation of indole derivatives as potent Kv1.5 inhibitors
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
چکیده انگلیسی
Atrial fibrillation (AF) is one of the common arrhythmias that threaten human health. Kv1.5 potassium channel is reported as an efficacious and safe target for the treatment of AF. In this paper, we designed and synthesized three series of compounds through modifying the lead compound RH01617 that was screened out by the pharmacophore model we reported earlier. All of the compounds were evaluated by the whole-patch lamp technology and most of them possessed potent inhibitory activities against Kv1.5. Compounds IIIi and IIIl were evaluated for the target selectivity as well as the pharmacodynamic effects in an isolated rat model. Due to the promising pharmacological behavior, compound IIIl deserves further pharmacodynamic and pharmacokinetic evaluations.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry - Volume 21, Issue 21, 1 November 2013, Pages 6466-6476
Journal: Bioorganic & Medicinal Chemistry - Volume 21, Issue 21, 1 November 2013, Pages 6466-6476
نویسندگان
Xiaoke Guo, Qian Yang, Jing Xu, Li Zhang, Hongxi Chu, Peng Yu, Yingying Zhu, Jinglian Wei, Weilin Chen, Yaozhong Zhang, Xiaojin Zhang, Haopeng Sun, Yiqun Tang, Qidong You,