Structure–activity relationship exploration of Kv1. 3 blockers based on diphenoxylate

…, BL Howard, DP Jenkins, H Wulff, PE Thompson…

Index: Nguyen, William; Howard, Brittany L.; Jenkins, David P.; Wulff, Heike; Thompson, Philip E.; Manallack, David T. Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 23 p. 7106 - 7109

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Citation Number: 4

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 ...