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 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.
Mahboobi
Siavosh
S
Department of Pharmaceutical Chemistry I, University of Regensburg, D-93040 Regensburg, Germany. siavosh.mahboobi@chemie.uni-regensburg.de
Eichhorn
Emerich
E
Popp
Alfred
A
Sellmer
Andreas
A
Elz
Sigurd
S
Möllmann
Ute
U
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D002939:Ciprofloxacin / Q000494:pharmacology; D004318:Doxycycline / Q000494:pharmacology; D004352:Drug Resistance, Microbial; D006094:Gram-Positive Bacteria / Q000187:drug effects*; D007211:Indoles / Q000138:chemical synthesis* / Q000494:pharmacology; D008826:Microbial Sensitivity Tests; D020102:Mycobacterium smegmatis / Q000187:drug effects; D011758:Pyrroles / Q000138:chemical synthesis* / Q000494:pharmacology; D013211:Staphylococcus aureus / Q000187:drug effects; D013329:Structure-Activity Relationship; D014640:Vancomycin / Q000494:pharmacology
D000900:Anti-Bacterial Agents; D007211:Indoles; D011758:Pyrroles; D002939:Ciprofloxacin; D014640:Vancomycin; D004318:Doxycycline