Pyruvate dehydrogenase complex E1 component (PDHc-E1) have been reported as potential target for agrochemical design, because it plays a pivotal role in cellular metabolism catalyzing the oxidative decarboxylation of pyruvate to acetyl-CoA, which is a critical step in the production of cellular energy. To identify novel antifungal lead compounds based on inhibitors of PDHc-E1, we have now designed series of PDHc-E1 inhibitors. In this poster, a series of novel 5-iodo-1,4-disubstituted-1,2,3-triazole derivatives (compound II ) were synthesized and evaluated their PDHc-E1 inhibitory activity and antifungal activity. The in vitro bioassay for PDHc-E1 inhibition indicated some compounds showed potent inhibitory activity. The antifungal activity results showed most compounds exhibited significant activity against Rhizoctonia solani and Botrytis cinerea at 100 �g/mL. Further antifungal evaluation indicted a compound exhibited almost 5.50-fold potency than Pyrimethani against Botrytis cinerea on the basis of EC50 and EC90. This implied that compound II  might be a potential fungicide leading structure for optimization.

Novel 5-iodo-1,4-disubstituted-1,2,3-triazole derivatives possessing potent antifungal activity as pyruvate dehydrogenase complex E1 inhibitors

248th National Meeting (2014)

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