Biopolym. Cell. 2026; 42(3):231-238.
https://doi.org/10.7124/bc.000BBD
Bioorganic Chemistry
Synthesis and antifungal activity of N-aryl-3,4-dichloromaleimides and N-substituted 3-chloro-4-aryloxymaleimides
1Tarnavskiy S. S., 1Borovykov O. V., 1Lukashov S. S., 1, 2Bieda O. A., 1Yarmoliuk S. M.
  1. Institute of Molecular Biology and Genetics, NAS of Ukraine
    150, Akademika Zabolotnoho Str., Kyiv, Ukraine, 03143
  2. LLC “Scientific and service firm “Otava”
    150, Akademika Zabolotnoho Str., Kyiv, Ukraine, 03143

Abstract

Aim. In the course of search for novel antimicrobials against the critical fungal pathogens a series of 3,4-dichloromaleimide and 3-chloro-4-aryloxymaleimide derivatives was synthesized. Methods. The structure of compounds was confirmed using 1H NMR spectroscopic analysis and LC-MS analysis. The antifungal assay was performed against Candida albicans and Cryptococcus neoformans as well as the cytotoxicity and hemolysis assays. Results. The compounds comparable with fluconazole in activity against C. neoformans were found in both classes: 3,4-dichloro-1-(2,4- dichlorophenyl)-2,5-dihydro-1H-pyrrole-2,5-dione showing minimum inhibitory concentration (MIC) 16 μg/mL (52 μmol/L) and 1-benzyl-3-chloro-4-(4-nitrophenoxy)-2,5-dihydro-1H-pyrrole-2,5-dione with MIC = 6 μg/mL (17 μmol/L). Conclusion. 3,4-dichloromaleimide and 3-chloro-4-aryloxymaleimide moieties were identified as a promising basis for the search for new antimicrobial agents active against C. albicans and C. neoformans.
Keywords: 3,4-dichloromaleimides, 3-chloro-4-aryloxymaleimides, antifungal activity, Cryptococcus neoformans, Candida albicans
Full text: (PDF, in English)

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