3-Bromo-4-(1H-3-indolyl)-2,5-dihydro-1H-2,5-pyrroledione derivatives as new lead compounds for antibacterially active substances

A number of new compounds containing 3-bromo-2,5-dihydro-1H-2,5-pyrroledione and indole substructures were found to have antibacterial activity against resistant strains of Staphylococcus aureus, Mycobacterium smegmatis and some other Gram positive bacteria. The investigated compounds exhibit minima...

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Bibliographic Details
Published in:European journal of medicinal chemistry 2006-02, Vol.41 (2), p.176-191
Main Authors: Mahboobi, Siavosh, Eichhorn, Emerich, Popp, Alfred, Sellmer, Andreas, Elz, Sigurd, Möllmann, Ute
Format: Article
Language:English
Subjects:
Anti-Bacterial Agents - chemical synthesis
Anti-Bacterial Agents - pharmacology
Ciprofloxacin - pharmacology
Doxycycline - pharmacology
Drug Resistance, Microbial
Gram-Positive Bacteria - drug effects
Indoles - chemical synthesis
Indoles - pharmacology
Microbial Sensitivity Tests
Mycobacterium smegmatis - drug effects
Pyrroles - chemical synthesis
Pyrroles - pharmacology
Staphylococcus aureus - drug effects
Structure-Activity Relationship
Vancomycin - pharmacology
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Summary:A number of new compounds containing 3-bromo-2,5-dihydro-1H-2,5-pyrroledione and indole substructures were found to have antibacterial activity against resistant strains of Staphylococcus aureus, Mycobacterium smegmatis and some other Gram positive bacteria. The investigated compounds exhibit minimal inhibition concentrations (MIC's) lower than those of ciprofloxacin, vancomycin and doxycycline resp. A different spectrum of activity, suggests a mechanism of action different to vancomycin and doxycycline. This might be important in circumventing existing resistance mechanisms. Here we report about the synthesis and on the antibacterial activity in a structure activity relationship study.
ISSN:0223-5234
DOI:10.1016/j.ejmech.2005.10.006