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Molecules ; 25(15)2020 Jul 31.
Article in English | MEDLINE | ID: mdl-32752024

ABSTRACT

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 1H-NMR, 13C-NMR and HRMS. The preliminary bioassay showed that most compounds had good larvicidal activities against mosquito larvae at 10 mg/L, especially compound 7a, 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 7h exhibited better inhibitory activity (90.5%) than fluxapyroxad (63.6%) against Botrytis cinereal. Therefore, this type of compound can be further studied.


Subject(s)
Benzamides/chemistry , Insecticides/chemical synthesis , Oxadiazoles/chemistry , Pyridines/chemistry , Animals , Antifungal Agents/chemical synthesis , Antifungal Agents/chemistry , Antifungal Agents/pharmacology , Botrytis/drug effects , Drug Design , Insecticides/chemistry , Insecticides/pharmacology , Larva/drug effects , Moths/drug effects , Moths/growth & development , Oxadiazoles/chemical synthesis , Oxadiazoles/pharmacology , Structure-Activity Relationship
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