title: Potentiating 1-(2-hydroxypropyl)-2-styryl-5-nitroimidazole derivatives against antibacterial agents: design, synthesis and biology analysis.
abstract: A series of novel 1-(2-hydroxypropyl)-2-styryl-5-nitroimidazole derivatives had been designed, synthesized, isolated and evaluated as potentiators of antibacterial agents. All these synthesized compounds were determined by elemental analysis, (1)H NMR, and MS. Their biological activities were also evaluated against two Gram-negative bacterial strains: Escherichia coli and Pseudomonas aeruginosa and two Gram-positive bacterial strains: Bacillus thuringiensis and Bacillus subtilis by MTT method as potential FabH inhibitory. The results showed that compound 30 exhibited the most potent E. coli FabH inhibitory activity with IC50 of 4.6 μM. Molecular modeling simulation studies were performed in order to predict the biological activities of the proposed compounds. All compounds have been tested for toxicity by MTT assay on human macrophage.
authors.affiliation: State Key Laboratory of Pharmaceutical Biotechnology, Nanjing University, Nanjing 210093, People's Republic of China.
authors.forename: Zhong-Chang
authors.initials: ZC
authors.lastname: Wang
authors.forename: Yong-Tao
authors.initials: YT
authors.lastname: Duan
authors.forename: Ya-Juan
authors.initials: YJ
authors.lastname: Qin
authors.forename: Peng-Fei
authors.initials: PF
authors.lastname: Wang
authors.forename: Yin
authors.initials: Y
authors.lastname: Luo
authors.forename: Qing
authors.initials: Q
authors.lastname: Wen
authors.forename: Yong-An
authors.initials: YA
authors.lastname: Yang
authors.forename: Juan
authors.initials: J
authors.lastname: Sun
authors.forename: Yang
authors.initials: Y
authors.lastname: Hu
authors.forename: Ya-Li
authors.initials: YL
authors.lastname: Sang
authors.forename: Hai-Liang
authors.initials: HL
authors.lastname: Zhu
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D001412:Bacillus subtilis / Q000187:drug effects*; D001413:Bacillus thuringiensis / Q000187:drug effects*; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D004926:Escherichia coli / Q000187:drug effects*; D006801:Humans; D008264:Macrophages; D008826:Microbial Sensitivity Tests; D008958:Models, Molecular; D015394:Molecular Structure; D009593:Nitroimidazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D011550:Pseudomonas aeruginosa / Q000187:drug effects*; D013329:Structure-Activity Relationship
chemical_list: C586342:1-(2-hydroxypropyl)-2-styryl-5-nitroimidazole; D000900:Anti-Bacterial Agents; D009593:Nitroimidazoles
keywords: Antibacterial activities; Cytotoxicity; FabH inhibitors; MTT assay; Nitroimidazole derivatives