کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
1368836 | 981729 | 2014 | 5 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
The discovery of benzenesulfonamide-based potent and selective inhibitors of voltage-gated sodium channel Nav1.7
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: The discovery of benzenesulfonamide-based potent and selective inhibitors of voltage-gated sodium channel Nav1.7 The discovery of benzenesulfonamide-based potent and selective inhibitors of voltage-gated sodium channel Nav1.7](/preview/png/1368836.png)
چکیده انگلیسی
The voltage gated sodium channel Nav1.7 represents an interesting target for the treatment of pain. Human genetic studies have identified the crucial role of Nav1.7 in pain signaling. Herein, we report the design and synthesis of a novel series of benzenesulfonamide-based Nav1.7 inhibitors. Structural–activity relationship (SAR) studies were undertaken towards improving Nav1.7 activity and minimizing CYP inhibition. These efforts resulted in the identification of compound 12k, a highly potent Nav1.7 inhibitor with a thousand-fold selectivity over Nav1.5 and negligible CYP inhibition.
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ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 24, Issue 18, 15 September 2014, Pages 4397–4401
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 24, Issue 18, 15 September 2014, Pages 4397–4401
نویسندگان
Shaoyi Sun, Qi Jia, Alla Y. Zenova, Mikhail Chafeev, Zaihui Zhang, Sophia Lin, Rainbow Kwan, Mike E. Grimwood, Sultan Chowdhury, Clint Young, Charles J. Cohen, Renata M. Oballa,