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Synthesis and biological activity of arylsulfonamide derivatives containing 2-arylamino-4(3H)-quinazolinone.

ABSTRACT: Twenty arylsulfonamide derivatives containing 2-arylamino-4(3H)-quinazolinone were synthesized and evaluated for their bioactivities. 4-Fluoro-N-(2-(4-oxo-2-(4-(trifluoromethoxy)phenyl)amino)quinazolin-3(4H)-yl)ethyl benzenesulfonamide, showed excellent activity both against Ralstonia solanacearum and Gibberella zeae with the inhibition rates of 100% (200?mg/L) and 95% (100?mg/L), and 69% (50?mg/L), respectively, exceeding that of the assigned commercial bactericide (thiodiazole-copper) and fungicide (hymexazol). The preliminary structure activity relationships (SAR) showed that both benzene rings of arylamino and arylsulfonamido moieties containing electron-withdrawing substitutes may be preferable for improving the bioactivity of target compounds.

SUBMITTER: Zeng Z

PROVIDER: S-EPMC6140676 | biostudies-literature | 2016 Nov

REPOSITORIES: biostudies-literature

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Synthesis and biological activity of arylsulfonamide derivatives containing 2-arylamino-4(3H)-quinazolinone.

Zeng Zhigang Z Gao Tao T Li Yan Y Wang Xiang X Yang Xuhong X Wu Minghu M

Journal of pesticide science 20161101 4

Twenty arylsulfonamide derivatives containing 2-arylamino-4(3H)-quinazolinone were synthesized and evaluated for their bioactivities. 4-Fluoro-N-(2-(4-oxo-2-(4-(trifluoromethoxy)phenyl)amino)quinazolin-3(4H)-yl)ethyl benzenesulfonamide, showed excellent activity both against Ralstonia solanacearum and Gibberella zeae with the inhibition rates of 100% (200 mg/L) and 95% (100 mg/L), and 69% (50 mg/L), respectively, exceeding that of the assigned commercial bacter ...[more]

PMID: 30363126

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