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  • Title: Design and synthesis of 2-styryl of 5-Nitroimidazole derivatives and antimicrobial activities as FabH inhibitors.
    Author: Duan YT, Wang ZC, Sang YL, Tao XX, Teraiya SB, Wang PF, Wen Q, Zhou XJ, Ding L, Yang YH, Zhu HL.
    Journal: Eur J Med Chem; 2014 Apr 09; 76():387-96. PubMed ID: 24594526.
    Abstract:
    A series of 2-Styryl-5-Nitroimidazole derivatives (25-48) have been synthesized and their biological activities were also evaluated against two Gram-negative bacterial strains: Escherichia coli and Pseudomonas aeruginosa and two Gram-positive bacterial strains: Bacillus subtilis and Bacillus thuringiensis as potential FabH inhibitors. All the compounds were structurally determined by (1)H NMR, MS, and elemental analysis. E. coli β-ketoacyl-acyl carrier protein synthase III inhibitory assay and docking simulation indicated that compound 33 with IC₅₀ of 9.0-36.4 μg/mL and compound 47 with IC₅₀ of 6.3-34.3 μg/mL against bacterial strains were most potent inhibitors of E. coli FabH. And more, compounds 33 and 47 which possessed a broad-spectrum of antibacterial activities didn't exhibit any toxicity towards macrophage.
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