Köksal Zeynep, Kalin Ramazan, Camadan Yasemin, Usanmaz Hande, Almaz Züleyha, Gülçin İlhami, Gokcen Taner, Gören Ahmet Ceyhan, Ozdemir Hasan
Department of Chemistry, Faculty of Sciences, İstanbul Medeniyet University, 34730 İstanbul, Turkey.
Department of Chemistry, Faculty of Science, Ataturk University, 25240 Erzurum, Turkey.
Molecules. 2017 May 24;22(6):793. doi: 10.3390/molecules22060793.
Secondary sulfonamides (-) 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 (-) were examined against LPO. The obtained results reveal that secondary sulfonamide derivatives (-) are effective LPO inhibitors. The K values of secondary sulfonamide derivatives (-) were found in the range of 1.096 × 10 to 1203.83 µM against LPO. However, the most effective inhibition was found for -(sulfathiazole)-3,4,5-triacetoxybenzamide (), with K values of 1.096 × 10 ± 0.471 × 10 µM as non-competitive inhibition.
合成了含有乙酰氧基苯甲酰胺、三乙酰氧基苯甲酰胺、羟基苯甲酰胺和三羟基苯甲酰胺并带有噻唑、嘧啶、吡啶、异恶唑和噻二唑基团的仲磺酰胺（-）。乳过氧化物酶（LPO，E.C.1.11.1.7）作为一种天然抗菌剂，是一种从唾液腺、乳腺和其他粘膜腺分泌的过氧化物酶。在本研究中，检测了一些仲磺酰胺衍生物（-）对LPO的体外抑制作用。所得结果表明仲磺酰胺衍生物（-）是有效的LPO抑制剂。仲磺酰胺衍生物（-）对LPO的K值在1.096×10至1203.83μM范围内。然而，发现-（磺胺噻唑）-3,4,5-三乙酰氧基苯甲酰胺（）的抑制作用最有效，其K值为1.096×10±0.471×10μM，为非竞争性抑制。
