Towards catalytic fluoroquinolones: from metal-catalyzed to metal-free DNA cleavage.

ABSTRACT: A library of eight new fluoroquinolone-nuclease conjugates containing a guanidinoethyl or aminoethyl auxiliary pendant on the 1,4,7-triazacyclononane (TACN) moiety was designed and synthesized to investigate their potential as catalytic antibiotics. The Cu(ii) complexes of the designer structures showed significant in vitro hydrolytic and oxidative DNA cleavage activity and good antibacterial activity against both Gram-negative and Gram-positive bacteria. The observed activity of all the Cu(ii)-TACN-ciprofloxacin complexes was strongly inhibited in the presence of Cu(ii)-chelating agents, thereby demonstrating "vulnerability" under physiological conditions. However, selected TACN-ciprofloxacin conjugates in their metal-free form efficiently cleaved plasmid DNA under physiological co

SUBMITTER: Goldmeier MN 

PROVIDER: S-EPMC11951297 | biostudies-literature | 2025 Jun

REPOSITORIES: biostudies-literature