Citation: Pan Dingwu, Du Huan, Lü Xinyang, Bao Xiaoping. Synthesis and Antibacterial Activities of Novel Quinazoline-2,4-dione Derivatives Containing the 1,2,4-Triazole Schiff-Base Unit[J]. Chinese Journal of Organic Chemistry, ;2016, 36(4): 818-825. doi: 10.6023/cjoc201510005 shu

Synthesis and Antibacterial Activities of Novel Quinazoline-2,4-dione Derivatives Containing the 1,2,4-Triazole Schiff-Base Unit

1.
State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Center for Research and Development of Fine Chemicals, Guizhou University, Guiyang 550025

Corresponding author: Bao Xiaoping,
Received Date: 9 October 2015
Available Online: 5 November 2015
Fund Project: 国家自然科学基金(No.21362003)资助项目. (No.21362003)

Eighteen novel quinazoline-2,4-dione derivatives containing the 1,2,4-triazole Schiff-base unit were designed and synthesized, based on the connection method of active fragments. Their structures were characterized by ¹H NMR, ¹³C NMR, MS, IR and elemental analysis. The preliminary antibacterial test indicated that all the target compounds possessed an excellent inhibition activity (≥ 93%) against Xanthomonas oryzae pv. oryzae (Xoo) at the concentration of 200 µg/mL, which was obviously better than those of control agents thiodiazole-copper and bismerthiazol. Compounds 7a, 7c~7g and 7j~7l still displayed 100% inhibition rate against Xoo even at the concentration of 100 µg/mL. Moreover, all the target compounds exhibited a certain inhibition activity against Xanthomonas axonopodis pv. citri, but no inhibition activity against Ralstonia solanacearum.
- 1,2,4-triazole Schiff-base,
- quinazoline-2,4-dione,
- synthesis,
- antibacterial activity
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