title: Exploration of structure-based on imidazole core as antibacterial agents.
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.
authors.forename: Yong-Tao
authors.initials: YT
authors.lastname: Duan
authors.forename: Zhong-Chang
authors.initials: ZC
authors.lastname: Wang
authors.forename: Ya-Li
authors.initials: YL
authors.lastname: Sang
authors.forename: Xiang-Xiang
authors.initials: XX
authors.lastname: Tao
authors.affiliation: School of Life Sciences, Nanjing University, Nanjing 210093, P. R. China. zhuhl@nju.edu.cn.
authors.forename: Hai-Liang
authors.initials: HL
authors.lastname: Zhu
mesh_terms: D015099:3-Oxoacyl-(Acyl-Carrier-Protein) Synthase; D000123:Acetyltransferases / Q000037:antagonists & inhibitors; D000591:Amino Acid Isomerases / Q000037:antagonists & inhibitors; D000900:Anti-Bacterial Agents / Q000737:chemistry* / Q000494:pharmacology*; D027081:DNA Gyrase / Q000378:metabolism; D027101:DNA Topoisomerase IV / Q000037:antagonists & inhibitors; D015195:Drug Design; D024901:Drug Resistance, Multiple, Bacterial; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology; D029968:Escherichia coli Proteins / Q000037:antagonists & inhibitors; D054889:Fatty Acid Synthase, Type II / Q000037:antagonists & inhibitors; D016480:Helicobacter pylori / Q000187:drug effects / Q000201:enzymology; D007093:Imidazoles / Q000737:chemistry*; D008826:Microbial Sensitivity Tests; D021281:Quantitative Structure-Activity Relationship; D059005:Topoisomerase II Inhibitors / Q000737:chemistry / Q000494:pharmacology; D014510:Urease / Q000037:antagonists & inhibitors; D065093:beta-Lactamase Inhibitors
chemical_list: D000900:Anti-Bacterial Agents; D004791:Enzyme Inhibitors; D029968:Escherichia coli Proteins; D007093:Imidazoles; D059005:Topoisomerase II Inhibitors; D065093:beta-Lactamase Inhibitors; C029899:imidazole; D000123:Acetyltransferases; C557158:fabH protein, E coli; D015099:3-Oxoacyl-(Acyl-Carrier-Protein) Synthase; D014510:Urease; D000591:Amino Acid Isomerases; C062292:glutamate racemase; D027101:DNA Topoisomerase IV; D027081:DNA Gyrase; D054889:Fatty Acid Synthase, Type II