Cyclam is a tetraazamacrocycle with applications in diverse fields of medicine. In particular, the bis-cyclam derivative AMD3100 was found to be a highly active and selective HIV inhibitor by interaction with the viral CXCR4 receptor. More recently, cyclam derivatives and their metal complexes revealed anticancer, antimalarial, antischistosomal and antimicrobial properties. The trans-disubstituted cyclam salt [H4{H2(4-CF3PhCH2)2Cyclam}]Cl4 revealed to be highly active against Escherichia coli and Staphylococcus aureus. However, the molecular interactions between cyclams and bacteria remains unknown until now. In this context, the cyclam-based Cu(II) complex [{H2(4-CF3PhCH2)2Cyclam}Cu(H2O)2](CH3COO)2 was synthesized, characterized, and used to gain insights into the cyclams' mechanism of action in bacteria. Carboxylic acid derivatized magnetic beads (Dynabeads Carboxylic Acid©) were chemically bonded to [{H2(4-CF3PhCH2)2Cyclam}Cu(H2O)2](CH3COO)2, to identify E. coli interacting proteins. The most recent results on the field will be presented and discussed.
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Insights into the antibacterial activity of cyclam derivatives
Published:
02 November 2021
by MDPI
in 7th International Electronic Conference on Medicinal Chemistry
session Round table on infectious diseases
Abstract:
Keywords: Cyclams, Copper(II) complexes, Antibacterials, E. coli, S. aureus
