Novel 5-methyl-2-phenylphenanthridium derivatives as FtsZ-targeting antibacterial agents from structural simplification of natural product sanguinarine.
Bioorg Med Chem Lett
; 28(10): 1825-1831, 2018 06 01.
Article
en En
| MEDLINE
| ID: mdl-29657101
ABSTRACT
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 7â¯l, 7m and 7n were found to display the most effective activity against five sensitive strains (0.06-2⯵g/mL) and three resistant strains (0.25-4⯵g/mL). The kinetic profiles indicated that compound 7l possessed the strongest bactericidal effect on S. aureus ATCC25923, with the MBC value of 16⯵g/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.
Palabras clave
Texto completo:
1
Banco de datos:
MEDLINE
Asunto principal:
Fenantridinas
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Proteínas Bacterianas
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Proteínas del Citoesqueleto
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Benzofenantridinas
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Isoquinolinas
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Antibacterianos
Idioma:
En
Año:
2018
Tipo del documento:
Article