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Synthesis and antifungal activity of 5-iodo-1,4-disubstituted-1,2,3-triazole derivatives as pyruvate dehydrogenase complex E1 inhibitors

文献类型： 外文期刊

作者： He, Jun-Bo 1 ; He, Hai-Feng 1 ; Zhao, Lu 1 ; Zhang, Li 1 ; You, Ge-Yun 1 ; Feng, Ling-Ling 1 ; Wan, Jian 1 ; He, Hong-Wu 1 ;

作者机构： 1.Cent China Normal Univ, Dept Chem, Minist Educ, Key Lab Pesticide & Chem Biol CCNU, Wuhan 430079, Peoples R China

2.Wuhan Polytech Univ, Coll Food Sci & Engn, Wuhan 430023, Peoples R China

3.Hubei Collaborat Innovat Ctr P

关键词： 5-Iodo-1;4-disubstituted-1;2;3-triazole;Pyruvate dehydrogenase complex;Inhibitor;Antifungal activity

期刊名称：BIOORGANIC & MEDICINAL CHEMISTRY （ 影响因子：3.641； 五年影响因子：3.319 ）

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收录情况： SCI

摘要： To identify new antifungal lead compound based on inhibitors of pyruvate dehydrogenase complex E1, a series of 5-iodo-1,4-disubstituted-1,2,3-triazole derivatives 3 were prepared and evaluated for their Escherichia coli PDHc-E1 inhibitory activity and antifungal activity. The in vitro bioassay for the PDHc-E1 inhibition indicated all the compounds exhibited significant inhibition against E. coli PDHc-E1 (IC50 < 21 mu M), special compound 3g showed the most potent inhibitory activity (IC50 = 4.21 +/- 0.11 mu M) and was demonstrated to act as a competitive inhibitor of PDHc-E1. Meanwhile, inhibitor 3g exhibited very good enzyme-selective inhibition of PDHc-E1 between pig heart and E. coli. The assay of antifungal activity showed compounds 3e, 3g, and 3n exhibited fair to good activity against Rhizoctonia solani and Botrytis cinerea even at 12.5 mu g/mL. Especially compound 3n (EC50 = 5.4 mu g/mL; EC90 = 21.1 mu g/mL) exhibited almost 5.50 times inhibitory potency against B. cinerea than that of pyrimethanil (EC50 = 29.6 mu g/mL; EC90 = 113.4 mu g/mL). Therefore, in this study, compound 3n was found to be a novel lead compound for further optimization to find more potent antifungal compounds as microbial PDHc-E1 inhibitors. (C) 2015 Elsevier Ltd. All rights reserved.

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