title: Synthesis and antibacterial activities of 1-alkyl-3-methacryloyl (acryloyl) of benzimidazolone (thione) derivatives.
abstract: A series of (28) 1-alkyl-3-methacryloyl (acryloyl)-benzimidazolone (thione) deriv-atives were synthesized. The structures of the new derivatives were confirmed by (1)H-NMR, (13)C-NMR and ESI-MS spectral analysis. The antibacterial activities of these compounds against several strains of bacteria, such as Bacillus cereus, Bacillus subtilis, Escherichia coli, Staphylococcus aureus and Pseudomonas aeruginosa, were evaluated by methods of paper disc-diffusion and broth mciro-dilution. Methacryloyl derivatives displayed higher antibacterial activities against tested bacterial strains than those of acryloyl derivatives in in vitro tests. A structure-activity relationship (SAR) study revealed that the presences of the methacryloyl moieties is essential to the antibacterial activities of the compounds.
authors.affiliation: College of plant protection and Institute of Pesticide Science, Northwest A & F University, Shaanxi 712100, China.
authors.forename: Shaopeng
authors.initials: S
authors.lastname: Wei
authors.affiliation: College of plant protection and Institute of Pesticide Science, Northwest A & F University, Shaanxi 712100, China.
authors.forename: Wenjun
authors.initials: W
authors.lastname: Wu
authors.affiliation: College of plant protection and Institute of Pesticide Science, Northwest A & F University, Shaanxi 712100, China.
authors.forename: Zhiqin
authors.initials: Z
authors.lastname: Ji
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D001562:Benzimidazoles / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D006090:Gram-Negative Bacteria / Q000187:drug effects*; D006094:Gram-Positive Bacteria / Q000187:drug effects*; D008826:Microbial Sensitivity Tests; D013329:Structure-Activity Relationship; D013871:Thiones / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology
chemical_list: D000900:Anti-Bacterial Agents; D001562:Benzimidazoles; D013871:Thiones; C014353:benzimidazolone