Citation: Tao Peng, Wenneng Wu. Syntheses and Antifungal Activities of 1, 3, 4-Oxadiazole (Thiadiazole) Derivatives Containing 4(3H)-Quinazolinone Moiety[J]. Chemistry, ;2021, 84(6): 604-609. shu

Syntheses and Antifungal Activities of 1, 3, 4-Oxadiazole (Thiadiazole) Derivatives Containing 4(3H)-Quinazolinone Moiety

Tao Peng ¹ ,
Wenneng Wu ^2,,

1.
Department of Brewing Engineering, Moutai Institute, Renhuai, 564500
2.
Food and Pharmaceutical Engineering Instituted, Guiyang University, Guiyang, 550005

Corresponding author: Wenneng Wu, wuwenneng123@126.com
Received Date: 4 December 2020
Accepted Date: 21 December 2020

Figures(1)

Using 2-aminobenzoic acid as raw material, ten 1, 3, 4-oxadiazole (thiadiazole) compounds containing quinazolin-4(3H)-one were synthesized through five step reactions including cyclization, condensation, hydrazinolysis, cyclization, thioetherification and oxidation. The structures of titled compounds were characterized by ¹H NMR, ¹³C NMR, MS and elemental analysis. The preliminary antifungal activity test indicated that the target compounds have moderate inhibitory activity against Botryosphaeria dothidea, Phomopsis sp. and B. cinerea at the concentration of 50μg/mL. The target compounds have good inhibitory activity against Pseudomonas syringae pv. actinidia, and the EC₅₀ values of compounds 6a and 6b against Pseudomonas syringae pv. actinidia are 11.7μg/mL and 20.5μg/mL, which are better than the control agent Bismerthiazol (24.5μg/mL). This kind of compounds have good biological activity for antibacterial. On this basis, the structure optimization is expected to find a compound with higher activity.
- Quinazolinone,
- 1, 3, 4-Oxadiazole,
- 1, 3, 4-Thiadiazole,
- Antibacterial activity
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