Vinsová Jarmila, Horák Václav, Buchta Vladimír, Kaustová Jarmila
Department of Inorganic and Organic Chemistry, Faculty of Pharmacy Charles University, 500 05 Hradec Králové, The Czech Republic.
Molecules. 2005 Aug 31;10(7):783-93. doi: 10.3390/10070783.
A series of lipophilic 2-substituted 5,7-di-tert-butylbenzoxazoles was prepared in average yields by the reaction of 3,5-di-tert-butyl-1,2-benzoquinone with amino acids and dipeptides bearing N-terminal glycine. Dipeptides having other N-terminal amino acids undergo oxidative deamination. 5,7-Di-tert-butylbenzoxazoles have shown activity against Mycobacterium tuberculosis and some nontuberculous strains where isoniazid has been inactive. Antifungal activity was mediocre.
通过3,5-二叔丁基-1,2-苯醌与带有N-末端甘氨酸的氨基酸和二肽反应，以平均产率制备了一系列亲脂性2-取代的5,7-二叔丁基苯并恶唑。具有其他N-末端氨基酸的二肽会发生氧化脱氨反应。5,7-二叔丁基苯并恶唑已显示出对结核分枝杆菌和一些异烟肼无活性的非结核菌株具有活性。抗真菌活性一般。
