The repeated application of fungicides with different modes of action is indispensable in current disease management programs to effectively control diseases and to delay the development of resistance in fungal plant pathogens. Fungicides can be applied in alternation or together in a mixture, the latter can be developed by a manufacturer as a co-formulation or prepared by the user as a tank mix. Although there are numerous advantages of using fungicide mixtures, their preparation requires more expert knowledge about the composition of single components and their incompatibility may lead to the loss of their efficacy. To avoid these drawbacks, our aim was to combine two fungicides with different modes of action into a single molecule, preserving its dual activity against both molecular targets of single fungicides. In particular, we covalently joined the pharmacophores of strobilurin- and succinate dehydrogenase inhibitor (SDHI) fungicides with a linker to obtain novel hybrid molecules. 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 activities confirmed dual mechanism of action of the new molecules. The dual-active molecules will be further optimized to increase their binding and inhibition of the two targets.

Designing dual-active fungicides for simultaneous inhibition of multiple target sites / A. Kunova, M. Zuccolo, F. Forlani, S.M.D. Dallavalle, P. Cortesi. - In: JOURNAL OF PLANT PATHOLOGY. - ISSN 2239-7264. - 101:(2019), pp. 828-829. ((Intervento presentato al 25. convegno Congress of the Italian Phytopathological Society tenutosi a Milano nel 2019 [10.1007/s42161-019-00394-4].

Designing dual-active fungicides for simultaneous inhibition of multiple target sites

A. Kunova
Primo
;
M. Zuccolo
Secondo
;
F. Forlani;S.M.D. Dallavalle;P. Cortesi
Ultimo
2019

Abstract

The repeated application of fungicides with different modes of action is indispensable in current disease management programs to effectively control diseases and to delay the development of resistance in fungal plant pathogens. Fungicides can be applied in alternation or together in a mixture, the latter can be developed by a manufacturer as a co-formulation or prepared by the user as a tank mix. Although there are numerous advantages of using fungicide mixtures, their preparation requires more expert knowledge about the composition of single components and their incompatibility may lead to the loss of their efficacy. To avoid these drawbacks, our aim was to combine two fungicides with different modes of action into a single molecule, preserving its dual activity against both molecular targets of single fungicides. In particular, we covalently joined the pharmacophores of strobilurin- and succinate dehydrogenase inhibitor (SDHI) fungicides with a linker to obtain novel hybrid molecules. 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 activities confirmed dual mechanism of action of the new molecules. The dual-active molecules will be further optimized to increase their binding and inhibition of the two targets.
Settore AGR/12 - Patologia Vegetale
Settore CHIM/08 - Chimica Farmaceutica
Settore BIO/10 - Biochimica
Article (author)
File in questo prodotto:
File Dimensione Formato  
2019-Kunova-JPP.pdf

accesso riservato

Tipologia: Publisher's version/PDF
Dimensione 2.01 MB
Formato Adobe PDF
2.01 MB Adobe PDF   Visualizza/Apri   Richiedi una copia
Pubblicazioni consigliate

Caricamento pubblicazioni consigliate

I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.

Utilizza questo identificativo per citare o creare un link a questo documento: http://hdl.handle.net/2434/710340
Citazioni
  • ???jsp.display-item.citation.pmc??? ND
  • Scopus ND
  • ???jsp.display-item.citation.isi??? 0
social impact