ethidium-homodimer-1 and sanguinarine

ethidium-homodimer-1 has been researched along with sanguinarine* in 2 studies

Other Studies

2 other study(ies) available for ethidium-homodimer-1 and sanguinarine

Article	Year
Novel 5-methyl-2-phenylphenanthridium derivatives as FtsZ-targeting antibacterial agents from structural simplification of natural product sanguinarine. Bioorganic & medicinal chemistry letters, 2018, 06-01, Volume: 28, Issue:10 A novel series of 5-methyl-2-phenylphenanthridium derivatives were displayed outstanding activity against a panel of antibiotic-sensitive and -resistant bacteria strains compared with their precursor sanguinarine, ciprofloxacin and oxacillin sodium. Compounds 7 l, 7m and 7n were found to display the most effective activity against five sensitive strains (0.06-2 μg/mL) and three resistant strains (0.25-4 μg/mL). The kinetic profiles indicated that compound 7l possessed the strongest bactericidal effect on S. aureus ATCC25923, with the MBC value of 16 μg/mL. The cell morphology and the FtsZ polymerization assays indicated that these compounds inhibited the bacterial proliferation by interfering the function of bacterial FtsZ. The SARs showed that all the 4-methyl-substituted 5-methyl-2-phenylphenanthridium subseries could be further investigated as the FtsZ-targeting antibacterial agents. Topics: Anti-Bacterial Agents; Bacterial Proteins; Benzophenanthridines; Binding Sites; Biological Products; Cytoskeletal Proteins; Drug Resistance, Bacterial; Gram-Negative Bacteria; Gram-Positive Bacteria; Isoquinolines; Microbial Sensitivity Tests; Molecular Dynamics Simulation; Phenanthridines; Protein Structure, Tertiary; Structure-Activity Relationship	2018
Antibacterial activity of substituted 5-methylbenzo[c]phenanthridinium derivatives. Bioorganic & medicinal chemistry letters, 2012, Dec-01, Volume: 22, Issue:23 Antibiotic resistance has prompted efforts to discover antibiotics with novel mechanisms of action. FtsZ is an essential protein for bacterial cell division, and has been viewed as an attractive target for the development of new antibiotics. Sanguinarine is a benzophenanthridine alkaloid that prevents cytokinesis in bacteria by inhibiting FtsZ self-assembly. In this study, a series of 5-methylbenzo[c]phenanthridinium derivatives were synthesized and evaluated for antibacterial activity against Staphylococcus aureus and Enterococcus faecalis. The data indicate that the presence of a 1- or 12-phenyl substituent on 2,3,8,9-tetramethoxy-5-methylbenzo[c]phenanthridinium chloride significantly enhances antibacterial activity relative to the parent compound or sanguinarine. Topics: Anti-Bacterial Agents; Bacterial Proteins; Benzophenanthridines; Cytoskeletal Proteins; Enterococcus faecalis; Isoquinolines; Microbial Sensitivity Tests; Phenanthridines; Staphylococcus aureus	2012

Article

Year

Novel 5-methyl-2-phenylphenanthridium derivatives as FtsZ-targeting antibacterial agents from structural simplification of natural product sanguinarine.

Bioorganic & medicinal chemistry letters, 2018, 06-01, Volume: 28, Issue:10

A novel series of 5-methyl-2-phenylphenanthridium derivatives were displayed outstanding activity against a panel of antibiotic-sensitive and -resistant bacteria strains compared with their precursor sanguinarine, ciprofloxacin and oxacillin sodium. Compounds 7 l, 7m and 7n were found to display the most effective activity against five sensitive strains (0.06-2 μg/mL) and three resistant strains (0.25-4 μg/mL). The kinetic profiles indicated that compound 7l possessed the strongest bactericidal effect on S. aureus ATCC25923, with the MBC value of 16 μg/mL. The cell morphology and the FtsZ polymerization assays indicated that these compounds inhibited the bacterial proliferation by interfering the function of bacterial FtsZ. The SARs showed that all the 4-methyl-substituted 5-methyl-2-phenylphenanthridium subseries could be further investigated as the FtsZ-targeting antibacterial agents.

Topics: Anti-Bacterial Agents; Bacterial Proteins; Benzophenanthridines; Binding Sites; Biological Products; Cytoskeletal Proteins; Drug Resistance, Bacterial; Gram-Negative Bacteria; Gram-Positive Bacteria; Isoquinolines; Microbial Sensitivity Tests; Molecular Dynamics Simulation; Phenanthridines; Protein Structure, Tertiary; Structure-Activity Relationship

2018

Antibacterial activity of substituted 5-methylbenzo[c]phenanthridinium derivatives.

Bioorganic & medicinal chemistry letters, 2012, Dec-01, Volume: 22, Issue:23

Antibiotic resistance has prompted efforts to discover antibiotics with novel mechanisms of action. FtsZ is an essential protein for bacterial cell division, and has been viewed as an attractive target for the development of new antibiotics. Sanguinarine is a benzophenanthridine alkaloid that prevents cytokinesis in bacteria by inhibiting FtsZ self-assembly. In this study, a series of 5-methylbenzo[c]phenanthridinium derivatives were synthesized and evaluated for antibacterial activity against Staphylococcus aureus and Enterococcus faecalis. The data indicate that the presence of a 1- or 12-phenyl substituent on 2,3,8,9-tetramethoxy-5-methylbenzo[c]phenanthridinium chloride significantly enhances antibacterial activity relative to the parent compound or sanguinarine.

Topics: Anti-Bacterial Agents; Bacterial Proteins; Benzophenanthridines; Cytoskeletal Proteins; Enterococcus faecalis; Isoquinolines; Microbial Sensitivity Tests; Phenanthridines; Staphylococcus aureus

2012