According to the superposition principle of reinforcement of biological activities, 24 novel 1,4- disubstituted phenyl-5-(halo-2-hydroxyphenyl)imino-l,2,3-triazoles was synthesized and characterized by 1H NMR, ^13C NMR, elemental analysis and IR. All the target compounds were screened for their antibacterial potential in vitro against Monilia albican, Escherichia coli and Staphylococcus aureus. It was shown that all the compounds possessed efficient antibacterial activities at a concentration of 0.1 mg/mL, even at a concentration of 0.01 mg/mL, some of the compounds still exhibited antibacterial activities against Escherichia coli and Monilia albican. At last, the struc- ture-activity relationship was discussed based on the antibacterial results.
ZHAO XuLU Jun-ruiXIN Chun-weiLU Bo-weiBAO Xiu-rongLI Jian-faLIU YaYANG Xu-yunYUAN Yi
A series of novel N-[(1-aryl-3-phenyl-pyrazol-4-yl)methylene]-2-(halo-o-hydroxyphenyl)hydrazide derivatives was synthesized and the antibacterial activity of each of them was evaluated. The supposed reaction mechanism of acquiring compounds 3a--3d is that catalytic activity is enhanced by the electron-donating groups of the first phenyl ring while decreased by electron-withdrawing groups of that ring. The result of preliminary bioassay shows that the lowest minimal inhibitory concentration(MIC) of the title compounds against Escherichia coli is 2 ℃g/mL. MIC values against Monilia albiean and Staphloeoeeus aureus are as low as 4 ~g/mL. They will be a series of potential antibacterial compounds against fungi and gram-negative bacteria.
LIU YaLU Bo-weiLU Jun-ruiXIN Chun-weiLI Jian-faMU Jiang-beiBAO Xiu-rong