Plant viral diseases cause the loss
of millions of dollars to agriculture
around the world annually. Therefore, the development of highly efficient,
ultra-low-dosage agrochemicals is desirable for protecting the health
of crops and ensuring food security. Herein, a series of 1,3,4-oxadiazole
derivatives bearing an isopropanol amine moiety was prepared, and
the inhibitory activity against tobacco mosaic virus (TMV) was assessed.
Notably, compound A14
exhibited excellent
anti-TMV protective activity with an EC50 value of 137.7
mg L–1, which was superior to that of ribavirin
(590.0 mg L–1) and ningnanmycin (248.2 mg L–1). Moreover, the anti-TMV activity of some compounds
could be further enhanced (by up to 5–30%) through supplementation
with 0.1% auxiliaries. Biochemical assays suggested that compound A14
could suppress the biosynthesis of TMV and
induce the plant’s defense response. Given these merits, designed
compounds had outstanding bioactivities and unusual action mechanisms
and were promising candidates for controlling plant viral diseases.
As quorum sensing (QS) regulates bacterial pathogenicity, antiquorum sensing agents have powerful application potential for controlling bacterial infections and overcoming pesticide/drug resistance. Identifying anti-QS agents thus represents a promising approach in agrochemical development. In this study, the anti-QS potency of 53 newly prepared benzothiazole derivatives containing an isopropanolamine moiety was analyzed, and structure−activity relationships were examined. Compound D 3 exhibited the strongest antibacterial activity, with an in vitro EC 50 of 1.54 μg mL −1 against Xanthomonas oryzae pv oryzae (Xoo). Compound D 3 suppressed QS-regulated virulence factors (e.g., biofilm, extracellular polysaccharides, extracellular enzymes, and flagella) to inhibit bacterial infection. In vivo anti-Xoo assays indicated good control efficiency (curative activity, 47.8%; protective activity, 48.7%) at 200 μg mL −1 . Greater control efficiency was achieved with addition of 0.1% organic silicone or orange peel essential oil. The remarkable anti-QS potency of these benzothiazole derivatives could facilitate further novel bactericidal compound development.
Anti-infection strategies based on suppression of bacterial virulence factors represent a crucial direction for the development of new antibacterial agents to address the resistance triggered by traditional drugs'/pesticides' bactericidal activity. To identify and obtain more effective and diverse molecules targeting virulence, we prepared a series of 3-hydroxy-2-methyl-1-pyridin-4-(1H)-one derivatives and evaluated their antibacterial behaviors. Compound B 6 exhibited the highest bioactivity, with half-maximal effective concentration (EC 50 ) values ranging fro9m 10.03 to 30.16 μg mL −1 against three plant pathogenic bacteria. The antibacterial mechanism showed that it could considerably reduce various virulence factors (such as extracellular enzymes, biofilm, and T3SS effectors) and inhibit the expression of virulence factor-related genes. In addition, the control efficiency of compound B 6 against rice bacterial leaf blight at 200 μg mL −1 was 46.15−49.15%, and their control efficiency was improved by approximately 12% after the addition of pesticide additives. Thus, a new class of bactericidal candidates targeting bacterial virulence factors was developed for controlling plant bacterial diseases.
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