Synthesis and fungicidal activity of 3,5-dichloropyrazin-2(1H)-one derivatives.
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.
François
Isabelle E J A
IE
Centre of Microbial and Plant Genetics, Katholieke Universiteit Leuven, Kasteelpark Arenberg 20, B-3001 Heverlee, Belgium.
Cammue
Bruno P A
BP
Bresseleers
Sara
S
Fleuren
Hein
H
Hoornaert
Georges
G
Mehta
Vaibhav P
VP
Modha
Sachin G
SG
Van der Eycken
Erik V
EV
Thevissen
Karin
K
D000935:Antifungal Agents / Q000494:pharmacology*; D002176:Candida albicans / Q000378:metabolism; D004247:DNA / Q000737:chemistry; D025141:Drug Resistance, Fungal / Q000187:drug effects; D005656:Fungal Proteins / Q000235:genetics / Q000378:metabolism; D017353:Gene Deletion; D016681:Genome, Fungal; D008826:Microbial Sensitivity Tests; D008956:Models, Chemical; D009154:Mutation; D011719:Pyrazines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D012441:Saccharomyces cerevisiae / Q000378:metabolism; D014617:Vacuoles / Q000737:chemistry
D000935:Antifungal Agents; D005656:Fungal Proteins; D011719:Pyrazines; D004247:DNA