Title: Design and Synthesis of a Series of Piperazine-1-carboxamidine Derivatives with Antifungal Activity Resulting from Accumulation of Endogenous Reactive Oxygen Species
Authors: François, I.E. ×
Thevissen, Karin
Pellens, Klaartje
Meert, Els
Heeres, J.
Freyne, E.
Croesemans, E.
Viellevoye, M.
Deroose, F.
Martinez Gonzalez, S.
Pastor, J.
Corens, D.
Meerpoel, L.
Borgers, M.
Ausma, J.
Dispersyn, G.D.
Cammue, Bruno #
Issue Date: 2009
Publisher: Wiley - V C H Verlag GmbH & Co. KGaA
Series Title: ChemMedChem vol:4 issue:10 pages:1714-1721
Abstract: In this study, we screened a library of 500 compounds for fungicidal activity via induction of endogenous reactive oxygen species (ROS) accumulation. Structure-activity relationship studies showed that piperazine-1-carboxamidine analogues with large atoms or large side chains substituted on the phenyl group at the R(3) and R(5) positions are characterized by a high ROS accumulation capacity in Candida albicans and a high fungicidal activity. Moreover, we could link the fungicidal mode of action of the piperazine-1-carboxamidine derivatives to the accumulation of endogenous ROS.
ISSN: 1860-7179
Publication status: published
KU Leuven publication type: IT
Appears in Collections:Centre of Microbial and Plant Genetics
× corresponding author
# (joint) last author

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