Selective Inhibition of Bacterial Topoisomerase I – IP 1330

Bacteria are rapidly evolving to be resistant tocurrently available antibiotics. In our fight against disease-causingpathogenic bacteria, it is crucial to synthesize compounds that can selectivelywork against bacteria while avoiding antibiotic resistance mechanisms. Enzymeinhibitors that selectively target bacterial enzymes, such as DNA topoisomerases (Topos),over their human equivalent offer a unique benefit in that regard.DNA Toposare enzymes responsible for the relaxation of (+) and (-) supercoiled (sc) DNA and the resolution of DNA knots and catenanes during essential biological processes, such as DNA replication, transcription, recombination, andmaintenance of chromosome structure.DNA Topos that control DNA topology inside cells are, thus, important targets for certain antibiotics and anticancer drugs. FIU scientists have synthesized Hoechst 33258 based bisbenzimidazoles containing aterminal hydrophobic group.These bisbenzimidazoles display topoisomerase I inhibition that is much betterthan Hoechst 33342 or Hoechst 33258, with IC50 values in the rangeof 2.47-6.63 μM. These compounds also display selective inhibition of E. coli topoisomerase I over DNA gyrase, human topoisomerases I and II, and effectivelyinhibit bacterial growth. Anne Laure Schmitt Olivier aschmitt@fiu.edu 305-348-5948

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