title: Synthesis of 1,2,3-triazole linked galactopyranosides and evaluation of cholera toxin inhibition.
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(50)s). Conversely, the monomeric galactotriazole analogues were strong inhibitors of cholera toxin (IC(50) = 71-75 μM).
authors: Department of Chemistry, La Trobe University, Victoria, 3086, Australia.
authors: David J
authors: DJ
authors: Leaver
authors: Raymond M
authors: RM
authors: Dawson
authors: Jonathan M
authors: JM
authors: White
authors: Anastasios
authors: A
authors: Polyzos
authors: Andrew B
authors: AB
authors: Hughes
mesh_terms: D002772:Cholera Toxin / Q000037:antagonists & inhibitors*; D005690:Galactose / Q000737:chemistry*; D015394:Molecular Structure; D013237:Stereoisomerism; D014230:Triazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*
chemical_list: D014230:Triazoles; D002772:Cholera Toxin; D005690:Galactose