Marine Josiane Minvielle

author keywords: Indole; Bacterial communication; Anti-virulence; Biofilm; Antibiotic resistance

TL;DR: An overview of the process controlled by indole signaling is given, current efforts to design indole-containing small molecules to intercept these pathways are summarized, and the synthetic efforts towards accessing indole derived bioactive small molecules are detailed. (via Semantic Scholar)

author keywords: desformylflustrabromine; mechanistic probes; natural products; phenotype control; structure-activity relationships

MeSH headings : Bacterial Proteins / antagonists & inhibitors; Bacterial Proteins / metabolism; Biofilms / drug effects; Gram-Negative Bacteria / drug effects; Gram-Negative Bacteria / physiology; Gram-Positive Bacteria / drug effects; Gram-Positive Bacteria / physiology; Hydrocarbons, Brominated / chemical synthesis; Hydrocarbons, Brominated / chemistry; Hydrocarbons, Brominated / pharmacology; Indole Alkaloids / chemical synthesis; Indole Alkaloids / chemistry; Indole Alkaloids / pharmacology; Indoles / chemical synthesis; Indoles / chemistry; Indoles / pharmacology; Phenotype; Structure-Activity Relationship; Temperature; Trans-Activators / antagonists & inhibitors; Trans-Activators / metabolism; Tryptophanase / antagonists & inhibitors; Tryptophanase / metabolism

TL;DR: This investigation demonstrates that molecules based on the dFBr scaffold can alter pathogenic behaviors by mimicking indole-signaling pathways and develop non-microbicidal dF Br derivatives that are 27-2000 times more active than indole in modulating biofilm formation, motility, acid resistance, and antibiotic resistance. (via Semantic Scholar)

TL;DR: Structural/function studies revealed that the addition of a bromine atom at the 2-position of the indole/triazole scaffold altered activity against both Gram-negative and Gram-positive bacteria and could transform a biofilm inhibitor into aBiofilm inducer. (via Semantic Scholar)

MeSH headings : Escherichia coli / metabolism; Hydrocarbons, Brominated / metabolism; Indole Alkaloids / metabolism; Indoles / metabolism; Signal Transduction; Staphylococcus aureus / metabolism

TL;DR: DFBr derivatives are found that are 10-1000 times more active than indole itself, demonstrating that the flustramine family of indolic natural products represent a privileged scaffold for the design of molecules to control pathogenic bacterial behavior. (via Semantic Scholar)