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Bioorg Med Chem Lett. 2014 Sep 28. pii: S0960-894X(14)01007-5. doi: 10.1016/j.bmcl.2014.09.054. [Epub ahead of print]

Design, synthesis and biological evaluation of metronidazole-thiazole derivatives as antibacterial inhibitors.

Author information

1
State Key Laboratory of Pharmaceutical Biotechnology, School of Life Science Nanjing University, Nanjing 210093, People's Republic of China.
2
School of Medicine, Nanjing University, Nanjing 210093, People's Republic of China.
3
State Key Laboratory of Pharmaceutical Biotechnology, School of Life Science Nanjing University, Nanjing 210093, People's Republic of China. Electronic address: zhuhl@nju.edu.cn.

Abstract

A series of metronidazole-thiazole derivatives has been designed, synthesized and evaluated as potential antibacterial inhibitors. All the synthesized compounds were determined by elemental analysis, 1H NMR and MS. They were also tested for antibacterial activity against Escherichia coli, Bacillus thuringiensis, Bacillus subtilis and Pseudomonas aeruginosa as well as for the inhibition to FabH. The results showed that compound 5e exhibited the most potent inhibitory activity against E. coli FabH with IC50 of 4.9μM. Molecular modeling simulation studies were performed in order to predict the biological activity of proposed compounds. Toxicity assay of compounds 5a, 5b, 5d, 5e, 5g and 5i showed that they were noncytotoxic against human macrophage. The results revealed that these compounds offered remarkable viability.

KEYWORDS:

Antibacterial activities; Cytotoxicity; FabH inhibitors; Metronidazole–thiazole derivatives; Molecule docking

PMID:
25318998
DOI:
10.1016/j.bmcl.2014.09.054

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