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https://doi.org/10.1038/s41598...
Article . 2019 . Peer-reviewed
License: CC BY
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https://www.nature.com/article...
Article
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Data sources: UnpayWall
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PubMed Central
Other literature type . 2019
Data sources: PubMed Central
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Dual-active antifungal agents containing strobilurin and SDHI-based pharmacophores

Authors: Zuccolo, Marco; Kunova, Andrea; Musso, Loana; Forlani, Fabio; Pinto, Andrea; Vistoli, Giulio; Gervasoni, Silvia; +2 Authors

Dual-active antifungal agents containing strobilurin and SDHI-based pharmacophores

Abstract

AbstractCrop disease management often implies repeated application of fungicides. However, the increasing emergence of fungicide-resistant pathogens requires their rotation or combined use. Tank-mix combinations using fungicides with different modes of action are often hard to manage by farmers. An alternative and unexploited strategy are bifunctional fungicides, i.e. compounds resulting from conjugation of the pharmacophores of fungicides with different mechanisms of action. In this paper we describe a new approach to antifungal treatments based on the synthesis of dual agents, obtained by merging the strobilurin and succinate dehydrogenase inhibitor pharmacophores into a new entity. The compounds were tested against important fungal plant pathogens and showed good inhibition of Pyricularia oryzae and Sclerotinia sclerotiorum with activity comparable to commercial fungicides. The inhibition of the cytochrome bc1 and the succinate dehydrogenase enzyme activity confirmed that the new molecules are endowed with a dual mechanism of action. These results were further supported by molecular modelling which showed that selected compounds form stable complexes with both cytochrome b subunit and succinate dehydrogenase enzyme. This work can be considered an important first step towards the development of novel dual-action agents with optimized structure and improved interaction with the targets.

Country
Italy
Related Organizations
Keywords

Antifungal Agents, Protein Conformation, Cytochromes b, Strobilurins, Article, Fungal Proteins, Molecular Docking Simulation, Succinate Dehydrogenase, Ascomycota, Drug Resistance, Fungal, Plant Diseases

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citations
This is an alternative to the "Influence" indicator, which also reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
BIP!Citations provided by BIP!
popularity
This indicator reflects the "current" impact/attention (the "hype") of an article in the research community at large, based on the underlying citation network.
BIP!Popularity provided by BIP!
influence
This indicator reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).
BIP!Influence provided by BIP!
impulse
This indicator reflects the initial momentum of an article directly after its publication, based on the underlying citation network.
BIP!Impulse provided by BIP!
22
Top 10%
Top 10%
Top 10%
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