Conventional-Microwave Mediated Synthesis and In Vitro Antimicrobial Activity of Novel Carbazole-Efflux Pump Inhibitor Hybrid Antibacterials

Work presented herein is the first report of two dual-action hybrids synthesized by covalent linkage of carbazole based novel antibacterial compounds with efflux pump inhibitors, that is, indole acetic acid/gallic acid. In this paper, novel antibacterial compounds 2 and 3 were prepared first and the...

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Main Authors: Ghazala Yaqub, Zubi Sadiq, Almas Hamid, Amber Fatima, Zainab Ijaz
Format: Article
Language:English
Published: Wiley 2017-01-01
Series:Journal of Chemistry
Online Access:http://dx.doi.org/10.1155/2017/7243279
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author Ghazala Yaqub
Zubi Sadiq
Almas Hamid
Amber Fatima
Zainab Ijaz
author_facet Ghazala Yaqub
Zubi Sadiq
Almas Hamid
Amber Fatima
Zainab Ijaz
author_sort Ghazala Yaqub
collection DOAJ
description Work presented herein is the first report of two dual-action hybrids synthesized by covalent linkage of carbazole based novel antibacterial compounds with efflux pump inhibitors, that is, indole acetic acid/gallic acid. In this paper, novel antibacterial compounds 2 and 3 were prepared first and then these were covalently linked with efflux pump inhibitors, that is, indole acetic acid/gallic acid leading to the successful formation of two dual-action hybrids 4 and 5. Prepared antibacterials and hybrids were evaluated for their bacteria cell killing capability against Escherichia coli, Staphylococcus aureus, Pasteurella multocida, and Bacillus subtilis. Both antibacterial compounds 2 and 3 were found effective against all tested bacterial strains at different concentrations. But when these compounds were linked with efflux pump inhibitors, they showed dramatic enhancement in their bacterial cell killing potential and minimum inhibitory concentration of all hybrids ranging from 7.250 μg/mL to 0.05 μg/mL. These prepared hybrid drugs will be promising and effective new agents in the category of dual-action antibiotics.
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id doaj-art-d6876baa858c47fe81573e3aeeecbb1c
institution Kabale University
issn 2090-9063
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language English
publishDate 2017-01-01
publisher Wiley
record_format Article
series Journal of Chemistry
spelling doaj-art-d6876baa858c47fe81573e3aeeecbb1c2025-02-03T01:23:20ZengWileyJournal of Chemistry2090-90632090-90712017-01-01201710.1155/2017/72432797243279Conventional-Microwave Mediated Synthesis and In Vitro Antimicrobial Activity of Novel Carbazole-Efflux Pump Inhibitor Hybrid AntibacterialsGhazala Yaqub0Zubi Sadiq1Almas Hamid2Amber Fatima3Zainab Ijaz4Department of Environmental Sciences, Kinnaird College for Women, Lahore 54000, PakistanLCWU, Lahore, PakistanDepartment of Environmental Sciences, Kinnaird College for Women, Lahore 54000, PakistanDepartment of Environmental Sciences, Kinnaird College for Women, Lahore 54000, PakistanDepartment of Environmental Sciences, Kinnaird College for Women, Lahore 54000, PakistanWork presented herein is the first report of two dual-action hybrids synthesized by covalent linkage of carbazole based novel antibacterial compounds with efflux pump inhibitors, that is, indole acetic acid/gallic acid. In this paper, novel antibacterial compounds 2 and 3 were prepared first and then these were covalently linked with efflux pump inhibitors, that is, indole acetic acid/gallic acid leading to the successful formation of two dual-action hybrids 4 and 5. Prepared antibacterials and hybrids were evaluated for their bacteria cell killing capability against Escherichia coli, Staphylococcus aureus, Pasteurella multocida, and Bacillus subtilis. Both antibacterial compounds 2 and 3 were found effective against all tested bacterial strains at different concentrations. But when these compounds were linked with efflux pump inhibitors, they showed dramatic enhancement in their bacterial cell killing potential and minimum inhibitory concentration of all hybrids ranging from 7.250 μg/mL to 0.05 μg/mL. These prepared hybrid drugs will be promising and effective new agents in the category of dual-action antibiotics.http://dx.doi.org/10.1155/2017/7243279
spellingShingle Ghazala Yaqub
Zubi Sadiq
Almas Hamid
Amber Fatima
Zainab Ijaz
Conventional-Microwave Mediated Synthesis and In Vitro Antimicrobial Activity of Novel Carbazole-Efflux Pump Inhibitor Hybrid Antibacterials
Journal of Chemistry
title Conventional-Microwave Mediated Synthesis and In Vitro Antimicrobial Activity of Novel Carbazole-Efflux Pump Inhibitor Hybrid Antibacterials
title_full Conventional-Microwave Mediated Synthesis and In Vitro Antimicrobial Activity of Novel Carbazole-Efflux Pump Inhibitor Hybrid Antibacterials
title_fullStr Conventional-Microwave Mediated Synthesis and In Vitro Antimicrobial Activity of Novel Carbazole-Efflux Pump Inhibitor Hybrid Antibacterials
title_full_unstemmed Conventional-Microwave Mediated Synthesis and In Vitro Antimicrobial Activity of Novel Carbazole-Efflux Pump Inhibitor Hybrid Antibacterials
title_short Conventional-Microwave Mediated Synthesis and In Vitro Antimicrobial Activity of Novel Carbazole-Efflux Pump Inhibitor Hybrid Antibacterials
title_sort conventional microwave mediated synthesis and in vitro antimicrobial activity of novel carbazole efflux pump inhibitor hybrid antibacterials
url http://dx.doi.org/10.1155/2017/7243279
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