Corrigendum to “Molecular and biological characterization of Sclerotinia sclerotiorum resistant to the anilinopyrimidine fungicide cyprodinil” [Pestic. Biochem. Physiol. 146 (2018) 80–89]

Hou, Yiping; Mao, Xuewei; Qu, Xiang-Pu; Wang, Jianxin; Chen, Changjun; Zhou, Mingguo

doi:10.1016/j.pestbp.2018.09.013

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“…Their activities were comparable to (or higher than) that of carbendazim (EC 50 = 0.21 μg/mL) . Furthermore, as a critical component of drugs/pesticides, the pyrimidine core is associated with antitumor, antifungal, herbicidal activities, etc. − More importantly, the pyrimidine core was also excavated as fungicides. For instance, pyrimethanil, dimethirimol, mepanipyrim, and cypro dinil (Figure ) are vital fungicides used in agriculture to combat fungal infections.…”

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confidence: 96%

Expanding the Structural Diversity of Tubulin-Targeting Agents: Development of Highly Potent Benzimidazoles for Treating Fungal Diseases

Yang,

Zhang,

et al. 2024

J. Agric. Food Chem.

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Benzimidazoles, the representative pharmacophore of fungicides, have excellent antifungal potency, but their simple structure and single site of action have hindered their wider application in agriculture. In order to extend the structural diversity of tubulin-targeted benzimidazoles, novel benzimidazole derivatives were prepared by introducing the attractive pyrimidine pharmacophore. 2-((6-(4-(trifluoromethyl)phenoxy)pyrimidin-4-yl)thio)-1H-benzo[d]imidazole (A 25 ) exhibited optimal antifungal activity against Sclerotinia sclerotiorum (S. s.), affording an excellent half-maximal effective concentration (EC 50 ) of 0.158 μg/mL, which was higher than that of the reference agent carbendazim (EC 50 = 0.594 μg/mL). Pot experiments revealed that compound A 25 (200 μg/mL) had acceptable protective activity (84.7%) and curative activity (78.1%), which were comparable with that of carbendazim (protective activity: 90.8%; curative activity: 69.9%). Molecular docking displayed that multiple hydrogen bonds and π−π interactions could be formed between A 25 and β-tubulin, resulting in a stronger bonding effect than carbendazim. Fluorescence imaging revealed that the structure of intracellular microtubules can be changed significantly after A 25 treatment. Overall, these remarkable antifungal profiles of constructed novel benzimidazole derivatives could facilitate the application of novel microtubuletargeting agents.

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