Antibacterial and Antifungal Activities of 2-(substituted ether)-5-(1-phenyl-5-(trifluoromethyl)-1H-pyrazol-4-yl)-1,3,4-oxadiazole Derivatives

作者：Zhang, Teng-Teng; Wang, Pei-Yi^*; Zhou, Jian; Shao, Wu-Bin; Fang, He-Shu; Zhou, Xiang; Wu, Zhi-Bing^*

来源：Journal of Heterocyclic Chemistry, 2017, 54(4): 2319-2325.

DOI：10.1002/jhet.2820

• BACTERIAL LEAF-BLIGHT
• IN-VITRO
• BIOLOGICAL-ACTIVITIES
• ANTIMICROBIAL AGENTS
• ANTICANCER ACTIVITY
• PYRAZOLE
• DESIGN
• MOIETY
• INHIBITORS
• BIOACTIVITIES

By replacing the amide bond into 1,3,4-oxadiazole moiety, a series of 1-phenyl-5-(trifluoromethyl)-1H-pyrazole derivatives bearing 1,3,4-oxadiazole were synthesized and evaluated their antibacterial and antifungal activity. The bioassay results revealed that compounds 7a and 7b showed the strongest antibacterial activity toward pathogen Xanthomonas oryzae pv. oryzae with the EC50 values of 15.0 and 6.4 mu g/mL, respectively; compound 6a exhibited comprehensive antifungal activity toward six kinds of fungi; compound 6f could selectively inhibit the growth of Sclertinia sclerotiorum and Rhizoctonia solani with the inhibition rates of 82.5 and 80.3% at the concentrate of 100 mu g/mL, respectively; compound 7b exerted good antifungal activity toward Fusarium oxysporum, Cytospora mandshurica, and Rhizoctonia solani with the inhibition rates of 70.8, 69.5, and 71.5%, respectively. The results suggested that this kind of compounds could be further studied as promising antimicrobial agents.

• 出版日期2017-7
• 单位贵州大学