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Secondary Sulfonamides as Effective Lactoperoxidase Inhibitors
Secondary sulfonamides (4a–8h) incorporating acetoxybenzamide, triacetoxybenzamide, hydroxybenzamide, and trihydroxybenzamide and possessing thiazole, pyrimidine, pyridine, isoxazole and thiadiazole groups were synthesized. Lactoperoxidase (LPO, E.C.1.11.1.7), as a natural antibacterial agent, is a...
Autores principales: | , , , , , , , , |
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Formato: | Online Artículo Texto |
Lenguaje: | English |
Publicado: |
MDPI
2017
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Materias: | |
Acceso en línea: | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6152724/ https://www.ncbi.nlm.nih.gov/pubmed/28538675 http://dx.doi.org/10.3390/molecules22060793 |
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author | Köksal, Zeynep Kalin, Ramazan Camadan, Yasemin Usanmaz, Hande Almaz, Züleyha Gülçin, İlhami Gokcen, Taner Gören, Ahmet Ceyhan Ozdemir, Hasan |
author_facet | Köksal, Zeynep Kalin, Ramazan Camadan, Yasemin Usanmaz, Hande Almaz, Züleyha Gülçin, İlhami Gokcen, Taner Gören, Ahmet Ceyhan Ozdemir, Hasan |
author_sort | Köksal, Zeynep |
collection | PubMed |
description | Secondary sulfonamides (4a–8h) incorporating acetoxybenzamide, triacetoxybenzamide, hydroxybenzamide, and trihydroxybenzamide and possessing thiazole, pyrimidine, pyridine, isoxazole and thiadiazole groups were synthesized. Lactoperoxidase (LPO, E.C.1.11.1.7), as a natural antibacterial agent, is a peroxidase enzyme secreted from salivary, mammary, and other mucosal glands. In the present study, the in vitro inhibitory effects of some secondary sulfonamide derivatives (4a–8h) were examined against LPO. The obtained results reveal that secondary sulfonamide derivatives (4a–8h) are effective LPO inhibitors. The K(i) values of secondary sulfonamide derivatives (4a–8h) were found in the range of 1.096 × 10(−3) to 1203.83 µM against LPO. However, the most effective inhibition was found for N-(sulfathiazole)-3,4,5-triacetoxybenzamide (6a), with K(i) values of 1.096 × 10(−3) ± 0.471 × 10(−3) µM as non-competitive inhibition. |
format | Online Article Text |
id | pubmed-6152724 |
institution | National Center for Biotechnology Information |
language | English |
publishDate | 2017 |
publisher | MDPI |
record_format | MEDLINE/PubMed |
spelling | pubmed-61527242018-11-13 Secondary Sulfonamides as Effective Lactoperoxidase Inhibitors Köksal, Zeynep Kalin, Ramazan Camadan, Yasemin Usanmaz, Hande Almaz, Züleyha Gülçin, İlhami Gokcen, Taner Gören, Ahmet Ceyhan Ozdemir, Hasan Molecules Article Secondary sulfonamides (4a–8h) incorporating acetoxybenzamide, triacetoxybenzamide, hydroxybenzamide, and trihydroxybenzamide and possessing thiazole, pyrimidine, pyridine, isoxazole and thiadiazole groups were synthesized. Lactoperoxidase (LPO, E.C.1.11.1.7), as a natural antibacterial agent, is a peroxidase enzyme secreted from salivary, mammary, and other mucosal glands. In the present study, the in vitro inhibitory effects of some secondary sulfonamide derivatives (4a–8h) were examined against LPO. The obtained results reveal that secondary sulfonamide derivatives (4a–8h) are effective LPO inhibitors. The K(i) values of secondary sulfonamide derivatives (4a–8h) were found in the range of 1.096 × 10(−3) to 1203.83 µM against LPO. However, the most effective inhibition was found for N-(sulfathiazole)-3,4,5-triacetoxybenzamide (6a), with K(i) values of 1.096 × 10(−3) ± 0.471 × 10(−3) µM as non-competitive inhibition. MDPI 2017-05-24 /pmc/articles/PMC6152724/ /pubmed/28538675 http://dx.doi.org/10.3390/molecules22060793 Text en © 2017 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 (CC BY) license (http://creativecommons.org/licenses/by/4.0/). |
spellingShingle | Article Köksal, Zeynep Kalin, Ramazan Camadan, Yasemin Usanmaz, Hande Almaz, Züleyha Gülçin, İlhami Gokcen, Taner Gören, Ahmet Ceyhan Ozdemir, Hasan Secondary Sulfonamides as Effective Lactoperoxidase Inhibitors |
title | Secondary Sulfonamides as Effective Lactoperoxidase Inhibitors |
title_full | Secondary Sulfonamides as Effective Lactoperoxidase Inhibitors |
title_fullStr | Secondary Sulfonamides as Effective Lactoperoxidase Inhibitors |
title_full_unstemmed | Secondary Sulfonamides as Effective Lactoperoxidase Inhibitors |
title_short | Secondary Sulfonamides as Effective Lactoperoxidase Inhibitors |
title_sort | secondary sulfonamides as effective lactoperoxidase inhibitors |
topic | Article |
url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6152724/ https://www.ncbi.nlm.nih.gov/pubmed/28538675 http://dx.doi.org/10.3390/molecules22060793 |
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