Structure-activity relationship exploration of Kv1.3 blockers based on diphenoxylate
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.
Nguyen, William,Howard, Brittany L.,Jenkins, David P.,Wulff, Heike,Thompson, Philip E.,Manallack, David T.
supporting information
p. 7106 - 7109
(2013/01/15)
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