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通过改良的 Gabriel-Cromwell 反应合成 2-氮丙啶基膦酸酯及其抗菌活性。

Synthesis of 2-aziridinyl phosphonates by modified Gabriel-Cromwell reaction and their antibacterial activities.

机构信息

Department of Chemistry, Middle East Technical University, 06531 Ankara, Turkey.

出版信息

Eur J Med Chem. 2011 Jun;46(6):2485-9. doi: 10.1016/j.ejmech.2011.03.037. Epub 2011 Apr 9.

Abstract

A set of new aziridinyl phosphonates (4a-g) were synthesized by using the Gabriel-Cromwell reaction and its modified version developed in this study and their structures confirmed by HRMS, IR, and NMR spectra. All the compounds were screened for their antibacterial activity. They all showed comparable moderate to good growth inhibitory activity in reference to ampicillin and streptomycin.

摘要

一套新的氮丙啶基膦酸盐(4a-g)通过 Gabriel-Cromwell 反应及其在本研究中开发的改良版本合成,并通过高分辨率质谱、红外和核磁共振谱确认其结构。所有化合物均进行了抗菌活性筛选。与氨苄西林和链霉素相比,它们均表现出相当中等至良好的生长抑制活性。

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