Department of Chemistry, Faculty of Science, Tarbiat Modares University, P.O. Box 14115-175, Tehran, Iran.
Eur J Med Chem. 2010 Nov;45(11):5130-9. doi: 10.1016/j.ejmech.2010.08.025. Epub 2010 Aug 18.
Some new phosphorus(V) hydrazides 1a-12a were synthesized and characterized by (1)H, (13)C, (31)P NMR, IR spectroscopy and elemental analysis. Moreover, the interaction of Cu(M)(2)·nH(2)O with 1a, 3a and 7a gave 4,4'-bis(morpholine)diazene (1b). In fact, in these reactions, copper(II) ions acted as oxidizing agent. The results supported the proposed mechanism. The structures of compounds 1a, 1b and 1c were further determined by X-ray crystallography. Compounds 1a-12a were screened for their antibacterial activities. Also, the acetyl- and butyrylcholinesterase inhibitory activity of 1a, 3a, 7a, 11a and 12a was measured using Ellman's method. It is interesting that these compounds were more potent inhibitors of BChE than of AChE. Also, using Lineweaver-Burk plots, it was indicated these compounds are mixed inhibitors.
一些新的磷（V）腙 1a-12a 通过 (1)H、(13)C、(31)P NMR、IR 光谱和元素分析进行了合成和表征。此外，Cu(M)(2)·nH(2)O 与 1a、3a 和 7a 的相互作用得到了 4,4'-双（吗啉）二氮杂环（1b）。实际上，在这些反应中，铜（II）离子充当了氧化剂。结果支持了所提出的机制。通过 X 射线晶体学进一步确定了化合物 1a、1b 和 1c 的结构。对化合物 1a-12a 进行了抗菌活性筛选。此外，使用 Ellman 法测量了 1a、3a、7a、11a 和 12a 的乙酰胆碱酯酶和丁酰胆碱酯酶抑制活性。有趣的是，这些化合物对 BChE 的抑制作用强于对 AChE 的抑制作用。此外，使用 Lineweaver-Burk 图表明这些化合物是混合抑制剂。
