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In Vitro Antimycobacterial Activity and Physicochemical Characterization of Diaryl Ether Triclosan Analogues as Potential InhA Reductase Inhibitors
Faculty
Pharmacy
Year:
2020
Type of Publication:
ZU Hosted
Pages:
3125
Authors:
Amany Mohamed Mohamed Elmahmoudy Sanger
Staff Zu Site
Abstract In Staff Site
Journal:
Molecules Mdpi
Volume:
Keywords :
, Vitro Antimycobacterial Activity and Physicochemical Characterization , Diaryl
Abstract:
Two sets of diphenyl ether derivatives incorporating five-membered 1,3,4-oxadiazoles, and their open-chain aryl hydrazone analogs were synthesized in good yields. Most of the synthesized compounds showed promising in vitro antimycobacterial activity against Mycobacterium tuberculosis H37Rv. Three diphenyl ether derivatives, namely hydrazide 3, oxadiazole 4 and naphthylarylidene 8g exhibited pronounced activity with minimum inhibitory concentrations (MICs) of 0.61, 0.86 and 0.99 g/mL, respectively compared to triclosan (10 g/mL) and isoniazid (INH) (0.2 g/mL). Compounds 3, 4, and 8g showed the InhA reductase enzyme inhibition with higher IC50 values (3.28–4.23 M) in comparison to triclosan (1.10 M). Correlation between calculated physicochemical parameters and biological activity has been discussed which justifies a strong correlation with respect to the inhibition of InhA reductase enzyme. Molecular modeling and drug-likeness studies showed good agreement with the obtained biological evaluation. The structural and experimental information concerning these three InhA inhibitors will likely contribute to the lead optimization of new antibiotics for M. tuberculosis.
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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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