Abstract
Defeat of the antibiotic resistance of pathogenic bacteria is one great challenge today and for the future. In the last century many classes of effective antibacterials have been developed, so that upcoming resistances could be met with novel drugs of various compound classes. Meanwhile, there is a certain lack of research of the pharmaceutical companies, and thus there are missing developments of novel antibiotics. Gram-positive bacteria are the most important cause of clinical infections. The number of novel antibacterials in clinical trials is strongly restricted. There is an urgent need to find novel antibacterials. We used synthetic chemistry to build completely novel hybrid molecules of substituted indoles and benzothiophene. In a simple one-pot reaction, two novel types of thienocarbazoles were yielded. Both indole substituted compound classes have been evaluated as completely novel antibacterials against the Staphylococcus and Enterococcus species. The evaluated partly promising activities depend on the indole substituent type. First lead compounds have been evaluated within in vivo studies. They confirmed the in vitro results for the new classes of small-molecule antibacterials.
Highlights
The increasing resistances of pathogenic bacteria are one great problem for worldwide health policy, because it means a threat of humanity [1]
Benzo[b]thiophenes have been reported to show antimicrobial activities depending on their substituents [20]
The formation of all those benzo[b]thiophene compounds started from a 3- or 7mostly halogen substituted benzo[b]thiophene scaffold which reacted with its 2-substituent to give
Summary
The increasing resistances of pathogenic bacteria are one great problem for worldwide health policy, because it means a threat of humanity [1]. They own promising properties for an oral use, and are not expected to show problems reported for those antimicrobial peptides [1]. Such small-molecule antibacterials that result from synthetic chemistry are unknown to emerge as a novel antibacterial compound class. Hybrid molecules of antimicrobial active antibiotics, or antifungal drugs have recently been reviewed [16,17] They mostly consist either of two different antibiotics or antifungals that are connected by a linker like a simple carbon chain. We identified first lead compounds with promising activities and confirmed the in vitro results first in the in vivo studies for selected derivatives
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