Antimicrobial cationic polyamines

摘要

Antimicrobial, non-hemolytic cationic polyamines were prepared by treating partially N-acylated polyethylenimines and/or partially oxidized polyethylenimines with a protic acid. The cationic polyamines can have a linear or branched polyethylenimine backbone structure. Preferably, the cationic polyamines comprise pendant urea groups, which can be introduced via a cyclic carbonate comprising a pendant urea group. The cationic polyamines can be active against a tuberculosis mycobacterium at low concentration. The cationic polyamines are also effective against Gram-negative Escherichia coli and Pseudomonas aeruginosa, Gram-positive Staphylococcus aureus, and fungus Candida albicans in solution and in the form of a film.

主权项

1. A method, comprising:
treating a medical condition caused by at least one bacterium by contacting the bacterium with a cationic polyamine, thereby killing the bacterium, wherein the cationic polyamine has a polymer backbone comprising:
i) a positive-charged first ethylenimine unit of formula (2):wherein X⊖ is a negative-charged counterion bound by non-covalent association with the positive charged nitrogen labeled 1, and
ii) a non-charged second ethylenimine unit of formula (3): wherein K′ comprises at least one carbon; and wherein no backbone nitrogen of the cationic polyamine is present as a quaternary ammonium salt, the cationic polyamine has a hemolysis HC20 value of greater than 1000 mg/L, and the first ethylenimine unit and the second ethylenimine unit of the polymer backbone are directly and/or indirectly covalently linked.