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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...

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Autores principales: Köksal, Zeynep, Kalin, Ramazan, Camadan, Yasemin, Usanmaz, Hande, Almaz, Züleyha, Gülçin, İlhami, Gokcen, Taner, Gören, Ahmet Ceyhan, Ozdemir, Hasan
Formato: Online Artículo Texto
Lenguaje:English
Publicado: MDPI 2017
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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.
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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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