新型双环硝基咪唑衍生物的合成、结构和生物评价。
Synthesis, structure and biological evaluation of novel bicyclic nitroimidazole derivatives.
机构信息
Pharmaceutical Faculty, Chair and Department of Organic Chemistry, Poznan University of Medical Sciences, Poznań, Poland.
出版信息
Arch Pharm (Weinheim). 2012 Jun;345(6):463-7. doi: 10.1002/ardp.201100379. Epub 2012 Jan 20.
A new series of 3-hydroxy-8-nitroimidazo[5,1-b]-1,4,5,6-tetrahydropyrimidine systems, being potential tuberculostatic agents, were synthesized. These products are close structural analogs of the basic structure of the known antitubercular bicyclic nitroimidazooxazine PA-824. The structures of the products obtained were confirmed by X-ray methods on the example of 3-hydroxy-8-nitro-1-phenylaminoimidazo[5,1-b]-1,4,5,6-tetrahydropyrimidine. Evaluation of these products for their anti-tuberculosis effects revealed interesting structure-activity relationships.
合成了一系列新的 3-羟基-8-硝基咪唑并[5,1-b]-1,4,5,6-四氢嘧啶系统，它们可能是潜在的抗结核药物。这些产物与已知的抗结核双环硝基咪唑嗪 PA-824 的基本结构非常相似。通过 X 射线方法，以 3-羟基-8-硝基-1-苯氨基咪唑并[5,1-b]-1,4,5,6-四氢嘧啶为例，证实了所得到的产物的结构。评估这些产物的抗结核效果揭示了有趣的构效关系。
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