Synthesis and Biological Activity of Benzamides Substituted with Pyridine-Linked 1,2,4-Oxadiazole.

MOLECULES(2020)

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摘要
To find pesticidal lead compounds with high activity, a series of novel benzamides substituted with pyridine-linked 1,2,4-oxadiazole were designed by bioisosterism, and synthesized easily via esterification, cyanation, cyclization and aminolysis reactions. The structures of the target compounds were confirmed by(1)H-NMR,C-13-NMR and HRMS. The preliminary bioassay showed that most compounds had good larvicidal activities against mosquito larvae at 10 mg/L, especially compound7a, with a larvicidal activity as high as 100%, and even at 1 mg/L was still 40%; at 50 mg/L, all the target compounds showed good fungicidal activities against the eight tested fungi. Moreover, compound7hexhibited better inhibitory activity (90.5%) than fluxapyroxad (63.6%) againstBotrytis cinereal. Therefore, this type of compound can be further studied.
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关键词
amide compound,fungicidal activity,insecticidal activity,1,2,4-oxadiazole,synthesis
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