Abstract
Nineteen N'-(benzylidene)-2-[(pyrimidin-2-yl)thio]acetohydrazides were obtained via the nucleophilic addition- elimination reaction of 2-[(pyrimidin-2-yl)thio)]acetohydrazide with aromatic aldehydes. The synthesized compounds were tested in vitro against various bacteria by microdilution. Among these compounds, N'-(3- hydroxybenzylidene)-2-[(pyrimidin-2-yl)thio]acetohydrazide (3l) was found to be the most potent derivative (MIC 7.8- 15.62 µg/mL) against Staphylococcus aureus (ATCC 6538), Staphylococcus epidermidis (ATCC 12228), and Escherichia coli (O157:H7-Clinical isolate), respectively. This outcome confirms that m-hydroxyphenyl moiety may have a considerable influence on antibacterial activity of the series tested. In the view of the results of the current work, further research can be carried out on the development of new effective antibacterial agents by the modification of compound 3l.
Keywords: Hydrazone, Pyrimidine, Antibacterial activity.
Letters in Drug Design & Discovery
Title:Synthesis and In Vitro Evaluation of Some Hydrazone Derivatives as Potential Antibacterial Agents
Volume: 11 Issue: 3
Author(s): Zafer Asim Kaplancikli, Mehlika Dilek Altintop, Ahmet Ozdemir, Gulhan Turan-Zitouni, Gamze Goger and Fatih Demirci
Affiliation:
Keywords: Hydrazone, Pyrimidine, Antibacterial activity.
Abstract: Nineteen N'-(benzylidene)-2-[(pyrimidin-2-yl)thio]acetohydrazides were obtained via the nucleophilic addition- elimination reaction of 2-[(pyrimidin-2-yl)thio)]acetohydrazide with aromatic aldehydes. The synthesized compounds were tested in vitro against various bacteria by microdilution. Among these compounds, N'-(3- hydroxybenzylidene)-2-[(pyrimidin-2-yl)thio]acetohydrazide (3l) was found to be the most potent derivative (MIC 7.8- 15.62 µg/mL) against Staphylococcus aureus (ATCC 6538), Staphylococcus epidermidis (ATCC 12228), and Escherichia coli (O157:H7-Clinical isolate), respectively. This outcome confirms that m-hydroxyphenyl moiety may have a considerable influence on antibacterial activity of the series tested. In the view of the results of the current work, further research can be carried out on the development of new effective antibacterial agents by the modification of compound 3l.
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Kaplancikli Asim Zafer, Altintop Dilek Mehlika, Ozdemir Ahmet, Turan-Zitouni Gulhan, Goger Gamze and Demirci Fatih, Synthesis and In Vitro Evaluation of Some Hydrazone Derivatives as Potential Antibacterial Agents, Letters in Drug Design & Discovery 2014; 11 (3) . https://dx.doi.org/10.2174/15701808113109990030
DOI https://dx.doi.org/10.2174/15701808113109990030 |
Print ISSN 1570-1808 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-628X |
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