Title:Exploration of Structure-Based on Imidazole Core as Antibacterial Agents
Volume: 13
Issue: 24
Author(s): Yong-Tao Duan, Zhong-Chang Wang, Ya-Li Sang, Xiang-Xiang Tao and Hai-Liang Zhu
Affiliation:
Keywords:
Antibacterial activity; antibacterial agents; docking; imidazole; kinase inhibitor; QSAR ; resistance to antibiotics;
structure-activity relationship.
Abstract: Imidazole, a five-membered heterocycle having three carbon atoms, and two double bonds, having efficient antibacterial
Escherichia coli, Bacillus subtili, Bacillus proteus, Staphylococcus aureus, Pseudomonas aeruginosa, and
Helicobacter pyloriurease etc, shows a broad-spectrum of antibacterial activities. To Search new antibacterial drugs to
overcome resistance of microorganisms to antibiotics, to date hundreds of this sort of derivatives have been synthesized
and possess potent antibacterial activity. As the structure of imidazole derivatives is various, the target of antibacterial is
also diverse including β-Lactamases, β-ketoacyl-acyl carrier protein synthase III (FabH), DNA gyrase and topoisomerase,
glutamate racemase and urease. In this review, we will discuss the emergence of resistance to antibiotics and attempt to
summarize the main developments of imidazole derivatives in the past ten years. We hope that increasing knowledge of
the structure-activity relationship (SAR) will be beneficial to the rational design of new generation of small molecule antibacterial
drugs.
