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

  作者 Francois, IEJA; Cammue, BPA; Bresseleers, S; Fleuren, H; Hoornaert, G; Mehta, VP; Modha, SG; Van der Eycken, EV; Thevissen, K  
  选自 期刊  Bioorganic & Medicinal Chemistry Letters;  卷期  2009年19-15;  页码  4064-4066  
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[摘要]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. (C) 2009 Elsevier Ltd. All rights reserved.

 
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