title: Synthesis and fungicidal activity of 3,5-dichloropyrazin-2(1H)-one derivatives.
abstract: 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.
authors: Centre of Microbial and Plant Genetics, Katholieke Universiteit Leuven, Kasteelpark Arenberg 20, B-3001 Heverlee, Belgium.
authors: Isabelle E J A
authors: IE
authors: François
authors: Bruno P A
authors: BP
authors: Cammue
authors: Sara
authors: S
authors: Bresseleers
authors: Hein
authors: H
authors: Fleuren
authors: Georges
authors: G
authors: Hoornaert
authors: Vaibhav P
authors: VP
authors: Mehta
authors: Sachin G
authors: SG
authors: Modha
authors: Erik V
authors: EV
authors: Van der Eycken
authors: Karin
authors: K
authors: Thevissen
mesh_terms: 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
chemical_list: D000935:Antifungal Agents; D005656:Fungal Proteins; D011719:Pyrazines; D004247:DNA