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Synthesis of 1,2,3-triazole linked galactopyranosides and evaluation of cholera toxin inhibition†
David J. Leaver,Raymond M. Dawson,Jonathan M. White,Anastasios Polyzos,Andrew B. Hughes
Organic & Biomolecular Chemistry Pub Date : 11/03/2011 00:00:00 , DOI:10.1039/C1OB06317K
Abstract

We report the synthesis of a series of bivalent 1,2,3-triazole linked galactopyranosides as potential inhibitors of cholera toxin (CT). The inhibitory activity of the bivalent series was examined (ELISA) and the series showed low inhibitory activity (millimolar IC50s). Conversely, the monomeric galactotriazole analogues were strong inhibitors of cholera toxin (IC50 = 71–75 μM).

Graphical abstract: Synthesis of 1,2,3-triazole linked galactopyranosides and evaluation of cholera toxin inhibition
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