کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10594356 | 981826 | 2012 | 4 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Structure-activity relationship exploration of Kv1.3 blockers based on diphenoxylate
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کلمات کلیدی
موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Structure-activity relationship exploration of Kv1.3 blockers based on diphenoxylate Structure-activity relationship exploration of Kv1.3 blockers based on diphenoxylate](/preview/png/10594356.png)
چکیده انگلیسی
Diphenoxylate, a well-known opioid agonist and anti-diarrhoeal agent, was recently found to block Kv1.3 potassium channels, which have been proposed as potential therapeutic targets for a range of autoimmune diseases. The molecular basis for this Kv1.3 blockade was assessed by the selective removal of functional groups from the structure of diphenoxylate as well as a number of other structural variations. Removal of the nitrile functional group and replacement of the C-4 piperidinyl substituents resulted in several compounds with submicromolar IC50 values.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 22, Issue 23, 1 December 2012, Pages 7106-7109
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 22, Issue 23, 1 December 2012, Pages 7106-7109
نویسندگان
William Nguyen, Brittany L. Howard, David P. Jenkins, Heike Wulff, Philip E. Thompson, David T. Manallack,