Design, Synthesis and Biological Activities of Novel Quinazolinone Derivatives Bearing 4-Phenyl-5-thioxo-1,2,4-triazole Mannich Bases

作者：Yan, Boren; Lu, Xinyang; Du, Huan; Bao, Xiaoping^*

来源：Chinese Journal of Organic Chemistry, 2016, 36(1): 207-212.

DOI：10.6023/cjoc201506026

• quinazolinone
• 1,2,4-triazole
• Mannich base
• antibacterial/antifungal activity

Using quinazolin-4-one as the starting compound, nine novel quinazolinone derivatives 6a similar to 6i bearing the 4-phenyl-5- thioxo-1,2,4-triazole Mannich base unit were prepared through a five-step synthetic procedure. The structures of target compounds were characterized by H-1 NMR, C-13 NMR, IR and elemental analysis. 34(1-Morpholinomethyl-4-phenyl-5-thioxo-4,5-dihydro-1H-1,2,4-triazol-3-yl)methyl)quinazolin-4(3H)-one was further confirmed by X-ray single crystal diffraction method. The preliminary biological test indicated that almost all of the title compounds had excellent antibacterial activities against Xanthomonas oryzae pv. oryzae and Xanthomonas axonopodis pv. citri at the concentration of 200 mu g/mL. Moreover, compounds 6a similar to 6i displayed a certain inhibitory effect against six kinds of tested fungi at the concentration of 50 mu g/mL.

• 出版日期2016-1
• 单位贵州大学