Cadelis, Melissa M.; Pike, Elliot I. W.; Kang, Weirong; Wu, Zimei; Bourguet-Kondracki, Marie-Lise; Blanchet, Marine; Vidal, Nicolas; Brunel, Jean Michel; Copp, Brent R. published the artcile< Exploration of the antibiotic potentiating activity of indolglyoxylpolyamines>, Quality Control of 93247-78-0, the main research area is bis indolyloxoacetamidopropyl butane diaminium trifluoroacetate preparation; antibacterial antifungal activity cytotoxicity SAR; Antimicrobial; Indole; Indolglyoxylamide; Polyamine; Potentiation.
A series of substituted di-indolglyoxylamido-spermine analogs I [R1 = 7-Me, 5-F, 5,6-di-Br, etc.] were prepared and evaluated for intrinsic antimicrobial properties and the ability to enhance antibiotic action. As a compound class, intrinsic activity was typically observed towards Gram-pos. bacteria and the fungus Cryptococcus neoformans, with notable exceptions being the compounds I [R1 = 5-Br, 5-Cl] analogs which also exhibited modest activity (MIC 34-50 μM) towards the Gram-neg. bacteria Escherichia coli and Klebsiella pneumoniae. Several analogs enhanced the activity of doxycycline towards the Gram-neg. bacteria Pseudomonas aeruginosa, E. coli, K. pneumoniae and Acinetobacter baumannii. Of particular note was the identification of five antibiotic enhancing analogs I [R1 = 5-Br, 7-F, 7-Me] which also exhibited low to no cytotoxicity and red blood cell haemolytic properties. The mechanisms of action of the I [R1 = 5-Br, 7-F] analogs were attributed to the ability to disrupt the integrity and depolarize, bacterial membranes.
European Journal of Medicinal Chemistry published new progress about Amines Role: ADV (Adverse Effect, Including Toxicity), PAC (Pharmacological Activity), RCT (Reactant), SPN (Synthetic Preparation), THU (Therapeutic Use), BIOL (Biological Study), RACT (Reactant or Reagent), PREP (Preparation), USES (Uses). 93247-78-0 belongs to class indole-building-block, and the molecular formula is C10H9NO2, Quality Control of 93247-78-0.
Referemce:
Indole alkaloid derivatives as building blocks of natural products from Bacillus thuringiensis and Bacillus velezensis and their antibacterial and antifungal activity study,
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles