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

DJ Leaver; RM Dawson; JM White; A Polyzos; AB Hughes

Journal article

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

DJ Leaver, RM Dawson, JM White, A Polyzos, AB Hughes

Organic and Biomolecular Chemistry | ROYAL SOC CHEMISTRY | Published : 2011

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 IC 50s). Conversely, the monomeric galactotriazole analogues were strong inhibitors of cholera toxin (IC 50 = 71-75 μM). © The Royal Society of Chemistry 2011.

University of Melbourne Researchers

Jonathan White Author

Anastasios Polyzos Author

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Grants

Funding Acknowledgements

DJL acknowledges the Australian Government for the provision of an Australian Postgraduate Award (APA) and La Trobe University/CSIRO for the La Trobe University/CSIRO Aurora PhD top-up Scholarship.