Synthesis, Anti-bacterial and Anti-oxidant Properties of Thiadiazaphosphol-2-ones
作者:Avula Balakrishna、Mudamala Veera Narayana Reddy、Sandip Kumar Nayak、Manubolu Manjunath、Chichili Devendranath Reddy、Cirandur Suresh Reddy
DOI:10.1248/cpb.56.1486
日期:——
4-Amino-5-phenyl-4H-1,2,4-triazole-3-thiol (1) underwent facile condensation with various phosphorus dichlorides (2a—j) in the presence of triethylamine in dry tetrahydrofuran at 60—65 °C and afforded corresponding thiadiazaphosphol-2-ones (3a—j). Their chemical structures were characterized using IR, 1H-, 13C-, 31P-NMR and Mass spectral studies. All the title compounds were screened for antioxidant properties by radical scavenging methods such as 1,1-diphenyl-2-picryl hydrazyl (DPPH), hydroxyl and lipid peroxidation. They exhibited potent in vitro antioxidant activity dose dependently. Their bioassay showed them to possess significant antibacterial activity.
4-氨基-5-苯基-4H-1,2,4-三唑-3-硫醇(1)在三乙胺存在下,与各种磷二氯化物(2a-j)在干燥四氢呋喃中60-65°C下进行便捷缩合反应,得到相应的硫代二氮磷杂环-2-酮(3a-j)。通过IR、1H-、13C-、31P-NMR和质谱研究表征了它们的化学结构。所有标题化合物通过1,1-二苯基-2-苦基肼(DPPH)、羟基和脂质过氧化等自由基清除方法进行了抗氧化性质筛选。它们表现出强有力的体外抗氧化活性,且活性随剂量变化。生物测定显示它们具有显著的抗菌活性。