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Design, synthesis, antimicrobial, and DNA gyrase inhibitory properties of fluoroquinolone–dichloroacetic acid hybrids
Faculty
Pharmacy
Year:
2020
Type of Publication:
ZU Hosted
Pages:
248–259
Authors:
Amany Mohamed Mohamed Elmahmoudy Sanger
Staff Zu Site
Abstract In Staff Site
Journal:
Chemical Biology and Drug Design Wiely
Volume:
Keywords :
Design, synthesis, antimicrobial, , , gyrase inhibitory properties , fluoroquinolone–dichloroacetic
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.
Author Related Publications
Amany Mohamed Mohamed Elmahmoudy Sanger, "Uracil as a Zn-Binding Bioisostere of the Allergic Benzenesulfonamide in the Design of Quinoline–Uracil Hybrids as Anticancer Carbonic Anhydrase Inhibitors", mdpi, 2022
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Amany Mohamed Mohamed Elmahmoudy Sanger, "Synthesis, Antibacterial Evaluation, and Computational Studies of a Diverse Set of Linezolid Conjugates", mdpi, 2022
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Amany Mohamed Mohamed Elmahmoudy Sanger, "Novel Benzyloxyphenyl Pyrimidine-5-Carbonitrile Derivatives as Potential Apoptotic Antiproliferative Agents", Bentham Science Publishers, 2022
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Amany Mohamed Mohamed Elmahmoudy Sanger, "DOCKING, SYNTHESIS AND BIOLOGICAL EVALUATION OF NOVEL PYRAZOLINE DERIVATIVES AS POTENTIAL ANTIMICROBIAL AND ANTITUMOR AGENTS", www.wjpr.net, 2016
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Amany Mohamed Mohamed Elmahmoudy Sanger, "SYNTHESIS OF NOVEL PYRIMIDINE AND FUSED PYRIMIDINE DERIVATIVES AND THEIR IN VITRO ANTIMICROBIAL AND CYTOTOXIC EVALUATION", www.wjpr.net, 2017
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Department Related Publications
Etedaal Hassan Mohamed Abdulaal, "18. In situ annelation of enaminones by reaction with methyleneiminium intermediates", لايوجد, 1900
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Hanan Abdelraziek Abdelfattah Ali Hamied, "synthesis of some new imidazolones of expected antimicrobial activity", لايوجد, 1900
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Azza Mohamed Kadry , "35. Synthesis and potentiometric study of some dioxadiaza ionophores in ion selective electrodes", لايوجد, 1900
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Azza Mohamed Kadry , "16. Chemistry of quinazolines: Reinvestigation of the action of hydrazine on thioxo derivatives", لايوجد, 1900
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Azza Mohamed Kadry , "2. Reaction and rearrangement of 2,4-quinazolinediones", لايوجد, 1900
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