Abstract
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.
Original language | English (US) |
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Pages (from-to) | 248-259 |
Number of pages | 12 |
Journal | Chemical Biology and Drug Design |
Volume | 95 |
Issue number | 2 |
DOIs | |
State | Published - Feb 1 2020 |
Keywords
- DNA gyrase
- antibacterial
- dichloroacetic acid
- fluoroquinolone
- hybrid conjugates
ASJC Scopus subject areas
- Biochemistry
- Molecular Medicine
- Pharmacology
- Drug Discovery
- Organic Chemistry