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Synthesis and Biological Activity of Benzamides Substituted with Pyridine-Linked 1,2,4-Oxadiazole
oleh: Sen Yang, Xiao-Yu Tian, Tian-Yang Ma, Li Dai, Chao-Li Ren, Jun-Chang Mei, Xing-Hai Liu, Cheng-Xia Tan
| Format: | Article |
|---|---|
| Diterbitkan: | MDPI AG 2020-07-01 |
Deskripsi
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 <sup>1</sup>H-NMR, <sup>13</sup>C-NMR and HRMS. The preliminary bioassay showed that most compounds had good larvicidal activities against mosquito larvae at 10 mg/L, especially compound <b>7a</b>, 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, compound <b>7h</b> exhibited better inhibitory activity (90.5%) than fluxapyroxad (63.6%) against <i>Botrytis cinereal</i>. Therefore, this type of compound can be further studied.