TY - JOUR
T1 - Undefeated-Changing the phenamacril scaffold is not enough to beat resistant Fusarium
AU - Wollenberg, Rasmus D.
AU - Donau, Søren S.
AU - Taft, Manuel H.
AU - Balázs, Zoltan
AU - Giese, Sven
AU - Thiel, Claudia
AU - Sørensen, Jens L.
AU - Nielsen, Thorbjørn T.
AU - Giese, Henriette
AU - Manstein, Dietmar J.
AU - Wimmer, Reinhard
AU - Sondergaard, Teis E.
PY - 2020/6
Y1 - 2020/6
N2 - Filamentous fungi belonging to the genus Fusarium are notorious plant-pathogens that infect, damage and contaminate a wide variety of important crops. Phenamacril is the first member of a novel class of single-site acting cyanoacrylate fungicides which has proven highly effective against important members of the genus Fusarium. However, the recent emergence of field-resistant strains exhibiting qualitative resistance poses a major obstacle for the continued use of phenamacril. In this study, we synthesized novel cyanoacrylate compounds based on the phenamacril-scaffold to test their growth-inhibitory potential against wild-type Fusarium and phenamacril-resistant strains. Our findings show that most chemical modifications to the phenamacril-scaffold are associated with almost complete loss of fungicidal activity and in vitro inhibition of myosin motor domain ATPase activity.
AB - Filamentous fungi belonging to the genus Fusarium are notorious plant-pathogens that infect, damage and contaminate a wide variety of important crops. Phenamacril is the first member of a novel class of single-site acting cyanoacrylate fungicides which has proven highly effective against important members of the genus Fusarium. However, the recent emergence of field-resistant strains exhibiting qualitative resistance poses a major obstacle for the continued use of phenamacril. In this study, we synthesized novel cyanoacrylate compounds based on the phenamacril-scaffold to test their growth-inhibitory potential against wild-type Fusarium and phenamacril-resistant strains. Our findings show that most chemical modifications to the phenamacril-scaffold are associated with almost complete loss of fungicidal activity and in vitro inhibition of myosin motor domain ATPase activity.
KW - Cyanoacrylates/pharmacology
KW - Drug Resistance, Fungal/drug effects
KW - Fungicides, Industrial/pharmacology
KW - Fusarium/drug effects
UR - http://www.scopus.com/inward/record.url?scp=85087326136&partnerID=8YFLogxK
U2 - 10.1371/journal.pone.0235568
DO - 10.1371/journal.pone.0235568
M3 - Journal article
C2 - 32598376
AN - SCOPUS:85087326136
SN - 1932-6203
VL - 15
JO - PLOS ONE
JF - PLOS ONE
IS - 6
M1 - e0235568
ER -