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Bioorg Med Chem Lett. 2009 Aug 1;19(15):4064-6. doi: 10.1016/j.bmcl.2009.06.024. Epub 2009 Jun 13.

Synthesis and fungicidal activity of 3,5-dichloropyrazin-2(1H)-one derivatives.

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  • 1Centre of Microbial and Plant Genetics, Katholieke Universiteit Leuven, Kasteelpark Arenberg 20, B-3001 Heverlee, Belgium.


We synthesized a family of 3,5-dichloropyrazin-2(1H)-one derivatives and assessed their in vitro fungicidal activity against Candida albicans. Compounds 11 and 20 were most active against C. albicans and induced accumulation of reactive oxygen species in this pathogen. Using a genome-wide approach in the yeast Saccharomyces cerevisiae, we demonstrated that genes involved in vacuolar functionality and DNA-related functions play an important role in cellular mechanisms underlying the fungicidal activity of these compounds.

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