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Design, synthesis, antimicrobial, and DNA gyrase inhibitory properties of fluoroquinolone–dichloroacetic acid hybrids
Author(s) -
Seliem Israa A.,
Panda Siva S.,
Girgis Adel S.,
Nagy Yosra I.,
George Riham F.,
Fayad Walid,
Fawzy Nehmedo G.,
Ibrahim Tarek S.,
AlMahmoudy Amany M. M.,
Sakhuja Rajeev,
Abdelsamii Zakaria K. M.
Publication year - 2020
Publication title -
chemical biology and drug design
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.59
H-Index - 77
eISSN - 1747-0285
pISSN - 1747-0277
DOI - 10.1111/cbdd.13638
Subject(s) - dna gyrase , enterococcus faecalis , escherichia coli , antimicrobial , chemistry , staphylococcus aureus , potency , minimum inhibitory concentration , combinatorial chemistry , microbiology and biotechnology , in vitro , biochemistry , stereochemistry , bacteria , biology , organic chemistry , gene , genetics
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.