title: Synthesis and antifungal evaluation of a series of maleimides.
abstract: 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.
  
  
  CONCLUSIONS
  The present work demonstrates that some maleimides can be used as potential lead compounds for developing novel antifungal agents against S. sclerotiorum.
authors.affiliation: Institute of Fermentation Engineering, College of Biological and Environmental Engineering, Zhejiang University of Technology, Hangzhou, China.
authors.forename: Xiao-Long
authors.initials: XL
authors.lastname: Chen
authors.forename: Li-Jun
authors.initials: LJ
authors.lastname: Zhang
authors.forename: Fu-Ge
authors.initials: FG
authors.lastname: Li
authors.forename: Yong-Xian
authors.initials: YX
authors.lastname: Fan
authors.forename: Wei-Ping
authors.initials: WP
authors.lastname: Wang
authors.forename: Bao-Ju
authors.initials: BJ
authors.lastname: Li
authors.forename: Yin-Chu
authors.initials: YC
authors.lastname: Shen
mesh_terms: D000935:Antifungal Agents / Q000138:chemical synthesis / Q000494:pharmacology; D001203:Ascomycota / Q000187:drug effects; D005659:Fungicides, Industrial / Q000138:chemical synthesis / Q000494:pharmacology*; D008301:Maleimides / Q000138:chemical synthesis / Q000494:pharmacology*; D008826:Microbial Sensitivity Tests; D013329:Structure-Activity Relationship
chemical_list: D000935:Antifungal Agents; D005659:Fungicides, Industrial; D008301:Maleimides
keywords: Sclerotinia sclerotiorum; antifungal agents; fungicide resistance; maleimides