1. Synthesis and biological activity of arylsulfonamide derivatives containing 2-arylamino-4(3H)-quinazolinone
- Author
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Yan Li, Tao Gao, Zhigang Zeng, Xuhong Yang, Minghu Wu, and Xiang Wang
- Subjects
Ralstonia solanacearum ,biology ,010405 organic chemistry ,Health, Toxicology and Mutagenesis ,Biological activity ,biology.organism_classification ,01 natural sciences ,Combinatorial chemistry ,Medicinal chemistry ,0104 chemical sciences ,010404 medicinal & biomolecular chemistry ,chemistry.chemical_compound ,Gibberella zeae ,chemistry ,Insect Science ,Antibacterial activity ,Benzene ,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.
- Published
- 2016