Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10594356 | Bioorganic & Medicinal Chemistry Letters | 2012 | 4 Pages |
Abstract
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.
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Authors
William Nguyen, Brittany L. Howard, David P. Jenkins, Heike Wulff, Philip E. Thompson, David T. Manallack,