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Antimicrobial Prospect of Newly Synthesized 1,3-Thiazole Derivatives
A new series of 1,3-thiazole and benzo[d]thiazole derivatives 10–15 has been developed, characterized, and evaluated for in vitro antimicrobial activity at concentrations of 25–200 μg/mL against Gram+ve organisms such as methicillin-resistant Staphylococcus aureus (MRSA), Gram–ve organisms such as E...
Autores principales: | , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
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MDPI
2011
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6264350/ https://www.ncbi.nlm.nih.gov/pubmed/22071446 http://dx.doi.org/10.3390/molecules16119386 |
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author | Sadek, Bassem Al-Tabakha, Moawia Mohammad Fahelelbom, Khairi Mustafa Salem |
author_facet | Sadek, Bassem Al-Tabakha, Moawia Mohammad Fahelelbom, Khairi Mustafa Salem |
author_sort | Sadek, Bassem |
collection | PubMed |
description | A new series of 1,3-thiazole and benzo[d]thiazole derivatives 10–15 has been developed, characterized, and evaluated for in vitro antimicrobial activity at concentrations of 25–200 μg/mL 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 11 and 12 showed notable antibacterial and antifungal activities at higher concentrations (125–200 μg/mL), whereas benzo[d]thiazole derivatives 13 and 14 were found to display significant antibacterial or antifungal activity (50–75 μg/mL) against the Gram+ve, Gram–ve bacteria, or fungal cells used in the present study. In addition, a correlation between calculated and determined partition coefficient (log P) was established which allows future development of compounds within this series to be carried out based on calculated log P values. Moreover, compounds 13 and 14 show that the optimum logarithm of partition coefficient (log P) should be around 4. |
format | Online Article Text |
id | pubmed-6264350 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2011 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-62643502018-12-10 Antimicrobial Prospect of Newly Synthesized 1,3-Thiazole Derivatives Sadek, Bassem Al-Tabakha, Moawia Mohammad Fahelelbom, Khairi Mustafa Salem Molecules Article A new series of 1,3-thiazole and benzo[d]thiazole derivatives 10–15 has been developed, characterized, and evaluated for in vitro antimicrobial activity at concentrations of 25–200 μg/mL 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 11 and 12 showed notable antibacterial and antifungal activities at higher concentrations (125–200 μg/mL), whereas benzo[d]thiazole derivatives 13 and 14 were found to display significant antibacterial or antifungal activity (50–75 μg/mL) against the Gram+ve, Gram–ve bacteria, or fungal cells used in the present study. In addition, a correlation between calculated and determined partition coefficient (log P) was established which allows future development of compounds within this series to be carried out based on calculated log P values. Moreover, compounds 13 and 14 show that the optimum logarithm of partition coefficient (log P) should be around 4. MDPI 2011-11-09 /pmc/articles/PMC6264350/ /pubmed/22071446 http://dx.doi.org/10.3390/molecules16119386 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 Al-Tabakha, Moawia Mohammad Fahelelbom, Khairi Mustafa Salem Antimicrobial Prospect of Newly Synthesized 1,3-Thiazole Derivatives |
title | Antimicrobial Prospect of Newly Synthesized 1,3-Thiazole Derivatives |
title_full | Antimicrobial Prospect of Newly Synthesized 1,3-Thiazole Derivatives |
title_fullStr | Antimicrobial Prospect of Newly Synthesized 1,3-Thiazole Derivatives |
title_full_unstemmed | Antimicrobial Prospect of Newly Synthesized 1,3-Thiazole Derivatives |
title_short | Antimicrobial Prospect of Newly Synthesized 1,3-Thiazole Derivatives |
title_sort | antimicrobial prospect of newly synthesized 1,3-thiazole derivatives |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6264350/ https://www.ncbi.nlm.nih.gov/pubmed/22071446 http://dx.doi.org/10.3390/molecules16119386 |
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