Synthesis and antifungal evaluation of a series of maleimides
2015
Chen, Xiao‐Long | Zhang, Li‐Jun | Li, Fu‐Ge | Fan, Yong‐Xian | Wang, Wei‐Ping | Li, Bao‐Ju | Shen, Yin‐Chu
BACKGROUND: Maleimides, both natural and synthesised, have good biological activities. In a continuous effort to discover new maleimides with good antifungal activities, the authors have synthesised a series of 3,4‐dichloro‐, 3‐methyl and non‐substituted maleimides based on previous studies. The compounds were biologically evaluated against the fungal pathogen Sclerotinia sclorotiorum. RESULTS: Of the 63 compounds evaluated, 25 compounds had interesting inhibitory potency with EC₅₀< 10 µg mL⁻¹. N‐(3,5‐Dichlorophenyl)‐3,4‐dichloromaleimide (EC₅₀= 1.11 µg mL⁻¹) and N‐octyl‐3‐methylmaleimide (EC₅₀= 1.01 µg mL⁻¹) were more potent than the commercial fungicide dicloran (EC₅₀= 1.72 µg mL⁻¹). The results showed that compounds exhibiting log P values within the range 2.4–3.0 displayed the best results in terms of fungicidal activity, and this seemed, therefore, to be the optimum range for this physicochemical parameter. CONCLUSION: The present work demonstrates that some maleimides can be used as potential lead compounds for developing novel antifungal agents against S. sclerotiorum. © 2014 Society of Chemical Industry
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