Synthesis of tetrazole compounds as a novel type of potential antimicrobial agents and their synergistic effects with clinical drugs and interactions with calf thymus DNA

被引:61
作者
Dai, Ling-Ling [1 ]
Zhang, Hui-Zhen [1 ]
Nagarajan, Sangaraiah [1 ]
Rasheed, Syed [1 ]
Zhou, Cheng-He [1 ]
机构
[1] Southwest Univ, Sch Chem & Chem Engn, Inst Bioorgan & Med Chem, Chongqing 400715, Peoples R China
基金
高等学校博士学科点专项科研基金; 中国国家自然科学基金;
关键词
BIOLOGICAL EVALUATION; BIOACTIVE EVALUATION; ANALOGS; ANTIBACTERIAL; BERBERINE; HYBRIDS; TRANSPORTATION; METRONIDAZOLE; SPECTROSCOPY; CHLOROMYCIN;
D O I
10.1039/c4md00266k
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
A series of tetrazole derivatives were synthesized and characterized by NMR, IR, MS and HRMS spectroscopy. The bioactive assay manifested that most of the target compounds exhibited good antifungal activity, especially compound 6g displayed comparable or even stronger antifungal efficiency in comparison with the reference drug Fluconazole. The combination of tetrazole derivative 6g with antibacterials Chloromycin and Norfloxacin, or antifungal Fluconazole respectively was more sensitive to methicillin-resistant MRSA and Fluconazole-insensitive Aspergillus flavus. Further research revealed that compound 6g could effectively intercalate into Calf Thymus DNA to form a 6g-DNA complex which might block DNA replication to exert its good antimicrobial activities.
引用
收藏
页码:147 / 154
页数:8
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