Walczak Krzysztof, Gondela Andrzej, Suwiński Jerzy
Department of Organic Chemistry, Biochemistry and Biotechnology, Silesian University of Technology, Krzywoustego 4, 44-100 Gliwice, Poland.
Eur J Med Chem. 2004 Oct;39(10):849-53. doi: 10.1016/j.ejmech.2004.06.014.
Twelve N-aryl derivatives of 4-nitroimidazole, 2-methyl-4-nitroimidazole, 4-nitropyrazole or 3-nitro-1,2,4-triazole have been synthesized either by a degenerated ring transformation reaction of 1,4-dinitroimidazoles with 4-substituted anilines or by a condensation of fluoronitrobenzenes with salts prepared from C-nitro-1H-azoles and 1,8-diazabicyclo[5.4.0]-7-undecene. The Tuberculosis Antimicrobial Acquisition and Coordinating Facility has provided anti-mycobacterial data concerning inhibition activity of 12 compounds.
通过1,4 - 二硝基咪唑与4 - 取代苯胺的退化环转化反应,或氟代硝基苯与由C - 硝基 - 1H - 唑和1,8 - 二氮杂双环[5.4.0]-7 - 十一碳烯制备的盐的缩合反应,合成了12种4 - 硝基咪唑、2 - 甲基 - 4 - 硝基咪唑、4 - 硝基吡唑或3 - 硝基 - 1,2,4 - 三唑的N - 芳基衍生物。结核病抗菌药物采购与协调机构提供了有关这12种化合物抑制活性的抗分枝杆菌数据。