Synthesis and fungicidal activity of 3,5-dichloropyrazin-2(1H)-one derivatives.
作者信息
François Isabelle E J A, Cammue Bruno P A, Bresseleers Sara, Fleuren Hein, Hoornaert Georges, Mehta Vaibhav P, Modha Sachin G, Van der Eycken Erik V, Thevissen Karin
机构信息
Centre of Microbial and Plant Genetics, Katholieke Universiteit Leuven, Kasteelpark Arenberg 20, B-3001 Heverlee, Belgium.
出版信息
Bioorg Med Chem Lett. 2009 Aug 1;19(15):4064-6. doi: 10.1016/j.bmcl.2009.06.024. Epub 2009 Jun 13.
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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