Synthesis and biological activities of novel quinazolinone derivatives containing a 1,2,4-triazolylthioether moiety |
| |
Authors: | Bo-Ren Yan Xin-Yang Lv Huan Du Man-Ni Gao Jian Huang Xiao-Ping Bao |
| |
Affiliation: | 1.State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering, Key Laboratory of Green Pesticide and Agricultural Bioengineering,Ministry of Education, Centre for Research and Development of Fine Chemicals, Guizhou University,Guiyang,China |
| |
Abstract: | A series of novel quinazolinone derivatives containing a 1,2,4-triazolylthioether moiety were synthesised and their antimicrobial activities were evaluated. All the target compounds were characterised by 1H NMR, 13C NMR, ESI-MS, IR and elemental analyses. The single crystal structure of 3-((5-((2-fluorobenzyl)thio)-4-phenyl-4H-1,2,4-triazol-3-yl)methyl)quinazolin-4(3H)-one (VIIi) was also determined. The preliminary bioassays indicated that some of the target compounds possessed good antimicrobial activities. For example, 3-((4-phenyl-5-((4-(trifluoromethyl)benzyl)thio)-4H-1,2,4-triazol-3-yl)methyl)quinazolin-4(3H)-one (VIIs) exhibited the best inhibitory effect against Xanthomonas oryzae pv. oryzae and Xanthomonas axonopodis pv. citri with the half-effective concentration (EC50) values of 47.6 μg mL?1 and 22.1 μg mL?1, respectively, which were superior to the commercial bactericide, bismerthiazol. Meanwhile, 3-((5-((4-chlorobenzyl)thio)-4-phenyl-4H-1,2,4-triazol-3-yl)methyl)quinazolin-4(3H)-one (VIIh) exhibited better fungicidal activities against Pellicularia sasakii and Colletotrichum capsici at the concentration of 50 μg mL?1, in comparison with the commercial fungicide, hymexazol. |
| |
Keywords: | |
本文献已被 SpringerLink 等数据库收录! |
|