Abstract
BackgroundPlant diseases seriously threaten food security, it is urgent to discover efficient and low-risk chemical pesticides. 1,2,4-Oxadiazole derivatives exhibit broad spectrum of agricultural biological activities. For discovering novel molecules with excellent agricultural activities, novel 1,2,4-oxadiazole derivatives were synthesized and evaluated for their agricultural activities.ResultBioassays results showed that the title compounds exhibited moderate nematocidal activity against Meloidogyne incognita and anti-fungal activity to Rhizoctonia solani. It’s worth noting that compounds 5m, 5r, 5u, 5v, 5x and 5y showed strong antibacterial effects on Xanthomonas oryzae pv. oryzae (Xoo), with EC50 values of 36.25, 24.14, 28.82, 19.44, 25.37 and 28.52 μg/mL, respectively, superior to bismerthiazol (BMT, EC50 = 77.46 μg/mL) and thiodiazole copper (TDC, EC50 = 99.31 μg/mL). Compounds 5p, 5u and 5v exhibited excellent antibacterial ability against Xanthomonas oryzae pv. oryzicola (Xoc), with EC50 values of 31.40, 19.04 and 21.78 μg/mL, respectively, better than that of BMT (EC50 = 68.50 μg/mL) and TDC (EC50 = 91.05 μg/mL). In addition, compound 5v exerted moderate antibacterial effects on rice bacterial leaf blight.ConclusionsTwenty-six novel 1,2,4-oxadiazole derivatives were obtained and their biological activities were evaluated. Compound 5u and 5v exhibited excellent antibacterial activity Xoo and Xoc. These results indicated that 1,2,4-oxadiazole derivatives containing a trifluoromethyl pyridine moiety could be as potential alternative templates for discovering novel antibacterial agents.
Highlights
Crop plants are constantly challenged by a wide variety of pathogens which threaten their growth and survival, such as bacteria, fungus, and plant-parasitic nematodes
Compound 5u and 5v exhibited excellent antibacterial activity Xanthomonas oryzae pv. oryzae (Xoo) and Xanthomonas oryzae pv. oryzicola (Xoc). These results indicated that 1,2,4-oxadiazole derivatives containing a trifluoromethyl pyridine moiety could be as potential alternative templates for discovering novel antibacterial agents
The literature survey reveals that fluopyram showed good antibacterial activity and nematocidal activity, and the important pharmacophore is trifluoromethyl pyridine moiety
Summary
Crop plants are constantly challenged by a wide variety of pathogens which threaten their growth and survival, such as bacteria, fungus, and plant-parasitic nematodes. As an important five-membered heterocyclic scaffold, 1,2,4-oxadiazoles, with good potent biological properties [20, 21] have been extensively used in pesticide and medicine [22,23,24] molecule design. 1,3,4-thiadiazol and 1,3,4-oxadiazole have been reported to have good biological activities and were used to design drug molecules in pesticide. We designed and synthesized a series of novel 1,3,4-thiadiazol and 1,3,4-oxadiazole derivatives with effective control of bacterial [25, 26], fungal [27,28,29] and plant-parasitic nematodes [30] diseases. Fluopyram, containing a trifluoromethyl pyridine moiety, is used for control of fungal diseases, and is used for control plant-parasitic nematodes disease [31, 32]. For discovering novel molecules with excellent agricultural activities, novel 1,2,4-oxadiazole derivatives were synthesized and evaluated for their agricultural activities
Sign-in/Register to view highlights & summary Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a callDisclaimer: All third-party content on this website/platform is and will remain the property of their respective owners and is provided on "as is" basis without any warranties, express or implied. Use of third-party content does not indicate any affiliation, sponsorship with or endorsement by them. Any references to third-party content is to identify the corresponding services and shall be considered fair use under The CopyrightLaw.
