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Synthesis, Characterization, and Antimicrobial Evaluation of Oxadiazole Congeners
A series of 1,3-oxazole, 1,3-thiazole, isomeric 1,2,4-oxadiazole, 1,3,4-oxadiazole, and 1,2,3,4-tetrazole heterocycles was synthesized. All the compounds shared as a common feature the presence of a 4-hydroxyphenyl substituent. The structures of the synthesized compounds were confirmed by MS, (1)H-N...
Autores principales: | , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2011
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6264570/ https://www.ncbi.nlm.nih.gov/pubmed/21613975 http://dx.doi.org/10.3390/molecules16064339 |
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author | Sadek, Bassem Fahelelbom, Khairi Mustafa Salem |
author_facet | Sadek, Bassem Fahelelbom, Khairi Mustafa Salem |
author_sort | Sadek, Bassem |
collection | PubMed |
description | A series of 1,3-oxazole, 1,3-thiazole, isomeric 1,2,4-oxadiazole, 1,3,4-oxadiazole, and 1,2,3,4-tetrazole heterocycles was synthesized. All the compounds shared as a common feature the presence of a 4-hydroxyphenyl substituent. The structures of the synthesized compounds were confirmed by MS, (1)H-NMR, and elemental analysis. In vitro antimicrobial activity for all the newly synthesized compounds at concentrations of 200-25 μg/mL was evaluated against Gram+ve organisms such as methicillin-resistant Staphylococcus aureus (MRSA), Gram–ve organisms such as Escherichia coli (E. coli), and the fungal strain Aspergillus niger (A. niger) by the cup plate method. Ofloxacin and ketoconazole (10 μg/mL) were used as reference standards for antibacterial and antifungal activity, respectively. Compounds 15, 16, and 20 showed notable antibacterial and antifungal activities at higher concentrations (200 μg/mL), whereas 17-19 were found to display significant antibacterial or antifungal activity (25-50 μg/mL) against the Gram+ve, Gram–ve bacteria, or fungal cells used in the present study. |
format | Online Article Text |
id | pubmed-6264570 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2011 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-62645702018-12-10 Synthesis, Characterization, and Antimicrobial Evaluation of Oxadiazole Congeners Sadek, Bassem Fahelelbom, Khairi Mustafa Salem Molecules Article A series of 1,3-oxazole, 1,3-thiazole, isomeric 1,2,4-oxadiazole, 1,3,4-oxadiazole, and 1,2,3,4-tetrazole heterocycles was synthesized. All the compounds shared as a common feature the presence of a 4-hydroxyphenyl substituent. The structures of the synthesized compounds were confirmed by MS, (1)H-NMR, and elemental analysis. In vitro antimicrobial activity for all the newly synthesized compounds at concentrations of 200-25 μg/mL was evaluated against Gram+ve organisms such as methicillin-resistant Staphylococcus aureus (MRSA), Gram–ve organisms such as Escherichia coli (E. coli), and the fungal strain Aspergillus niger (A. niger) by the cup plate method. Ofloxacin and ketoconazole (10 μg/mL) were used as reference standards for antibacterial and antifungal activity, respectively. Compounds 15, 16, and 20 showed notable antibacterial and antifungal activities at higher concentrations (200 μg/mL), whereas 17-19 were found to display significant antibacterial or antifungal activity (25-50 μg/mL) against the Gram+ve, Gram–ve bacteria, or fungal cells used in the present study. MDPI 2011-05-25 /pmc/articles/PMC6264570/ /pubmed/21613975 http://dx.doi.org/10.3390/molecules16064339 Text en © 2011 by the authors; licensee MDPI, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/3.0/). |
spellingShingle | Article Sadek, Bassem Fahelelbom, Khairi Mustafa Salem Synthesis, Characterization, and Antimicrobial Evaluation of Oxadiazole Congeners |
title | Synthesis, Characterization, and Antimicrobial Evaluation of Oxadiazole Congeners |
title_full | Synthesis, Characterization, and Antimicrobial Evaluation of Oxadiazole Congeners |
title_fullStr | Synthesis, Characterization, and Antimicrobial Evaluation of Oxadiazole Congeners |
title_full_unstemmed | Synthesis, Characterization, and Antimicrobial Evaluation of Oxadiazole Congeners |
title_short | Synthesis, Characterization, and Antimicrobial Evaluation of Oxadiazole Congeners |
title_sort | synthesis, characterization, and antimicrobial evaluation of oxadiazole congeners |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6264570/ https://www.ncbi.nlm.nih.gov/pubmed/21613975 http://dx.doi.org/10.3390/molecules16064339 |
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