TY  - JOUR
A1  - Ashraf, Kerolos
A1  - Yasrebi, Kaveh
A1  - Hertlein, Tobias
A1  - Ohlsen, Knut
A1  - Lalk, Michael
A1  - Hilgeroth, Andreas
T1  - Novel effective small-molecule antibacterials against \(Enterococcus\) strains
JF  - Molecules
N2  - \(Enterococcus\) species cause increasing numbers of infections in hospitals. They contribute to the increasing mortality rates, mostly in patients with comorbidities, who suffer from severe diseases. \(Enterococcus\) resistances against most antibiotics have been described, including novel antibiotics. Therefore, there is an ongoing demand for novel types of antibiotics that may overcome bacterial resistances. We discovered a novel class of antibiotics resulting from a simple one-pot reaction of indole and \(o\)-phthaldialdehyde. Differently substituted indolyl benzocarbazoles were yielded. Both the indole substitution and the positioning at the molecular scaffold influence the antibacterial activity towards the various strains of \(Enterococcus\) species with the highest relevance to nosocomial infections. Structure-activity relationships are discussed, and the first lead compounds were identified as also being effective in the case of a vancomycin resistance.
KW  - medicine
KW  - antibacterial activity
KW  - synthesis
KW  - derivatives
KW  - structure-activity
KW  - lead structure
Y1  - 2017
U6  - http://nbn-resolving.de/urn/resolver.pl?urn:nbn:de:bvb:20-opus-172628
VL  - 22
IS  - 12
ER  -