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Synthesis and biological evaluation of Schiff base-linked imidazolyl naphthalimides as novel potential anti-MRSA agents
被引:48
|作者:
Gong, Huo-Hui
[1
]
Baathulaa, Kishore
[1
]
Lv, Jing-Song
[1
]
Cai, Gui-Xin
[1
]
Zhou, Cheng-He
[1
]
机构:
[1] Southwest Univ, Sch Chem & Chem Engn, Key Lab Appl Chem Chongqing Municipal, Inst Bioorgan & Med Chem, Chongqing 400715, Peoples R China
来源:
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:
CALF THYMUS DNA;
ANTIMICROBIAL AGENTS;
BIOACTIVE EVALUATION;
ANTIBACTERIAL;
DESIGN;
DERIVATIVES;
AZOLES;
METRONIDAZOLE;
ANTICANCER;
QUINOLONES;
D O I:
10.1039/c5md00574d
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 novel Schiff base-linked imidazole naphthalimides were developed and their antimicrobial behavior demonstrated that compound 9i could effectively inhibit the growth of some tested strains, especially for MRSA (MIC = 0.003 mu mol mL(-1)), which was superior to the reference drugs. Bacterial membrane permeabilization, bacterial resistance and time-kill kinetic assays of compound 9i against MRSA manifested that it was able to permeate the cell membrane, rapidly kill the tested strains and stall the development of bacterial resistance. Preliminary research revealed that compound 9i could form a stable complex with calf thymus DNA by intercalation mode. These results suggested that compound 9i could serve as a promising anti-MRSA candidate.
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页码:924 / 931
页数:8
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