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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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Detalles Bibliográficos
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
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
Descripción
Sumario: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.