Zeng, Jie; Zhang, Zhijun; Zhu, Qi; Jiang, Zhiyan; Zhong, Guohua published the artcile< Simplification of natural β-carboline alkaloids to obtain indole derivatives as potent fungicides against rice sheath blight>, Safety of 2-(Trifluoromethoxy)benzoyl chloride, the main research area is indole preparation Agrochem fungicide SAR; Rhizoctonia solani; fungicidal activity; indole; simplification; β-carboline.
The increasing resistance of rice sheath blight caused by Rhizoctonia solani highlights the need for highly effective and environmentally benign agents. Natural β-carboline alkaloids were simplified to obtain a series of indole derivatives, and their fungicidal activity and preliminary mode of action against R. solani were also evaluated. The initial hit indole displayed significant fungicidal activity with an EC50 value of 25.56μg/mL, and was selected for further optimization. Importantly, compound 4-fluroindole the most active compound, had an EC50 value of 0.62μg/mL, and approx. 300-fold more potent than validamycin A (EC50 = 183.00μg/mL). In-vivo bioassay also demonstrated that compound 4-fluoroindole showed better fungicidal activities than validamycin A. Moreover, the mechanism studies revealed that compound 4-fluoroindole not only caused remarkable morphol. and structural alterations of R. solani hyphae, but also induced the loss of mitochondrial membrane potential and interfered with DNA synthesis. Therefore, compound 4-fluoroindole showed superior fungicidal activity against R. solani, and the elucidated mode of action supported the potential application of compound 4-fluoroindole against rice sheath blight.
Molecules published new progress about Agrochemical fungicides. 162046-61-9 belongs to class chlorides-buliding-blocks, and the molecular formula is C8H4ClF3O2, Safety of 2-(Trifluoromethoxy)benzoyl chloride.
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Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics