Journal
CHEMICAL BIOLOGY & DRUG DESIGN
Volume 95, Issue 2, Pages 248-259Publisher
WILEY
DOI: 10.1111/cbdd.13638
Keywords
antibacterial; dichloroacetic acid; DNA gyrase; fluoroquinolone; hybrid conjugates
Funding
- Egyptian Cultural and Educational Bureau Scholarship
- Center for Undergraduate Research and Scholarship (CURS) at Augusta University
- Translational Research Program (TRP) at Augusta University
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A series of new fluoroquinolone conjugates 8a-g and 9a-f were synthesized via benzotriazole-mediated synthetic approach with good yield and purity. Some of the synthesized analogs exhibited significant antibacterial properties against Escherichia coli and Staphylococcus aureus with potency higher than that of the parent drugs through in vitro standard bioassay procedure (conjugates 8c and 8d reveal antimicrobial properties with potency 1.9, 61.9, 20.7 and 2.4, 37.1, 8.3 folds relative to the parent antibiotic 6 against E. coli, S. aureus, and Enterococcus faecalis, respectively). The observed experimental data were supported by enzymatic DNA gyrase inhibitory property. Developed BMLR-QSAR model validates the observed experimental data and recognizes the parameters responsible for the enhanced antibacterial properties.
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