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在对氨基糖苷类的改造中,试用碱性较强的基因取代氨基以增强其化合物的碱性,这样即能提高药物的抗菌活性,又不致于使毒性增强,为此合成了一系列1-N-[4-(取代)脒基/胍基2-羟丁酰基]卡那霉素 A 和 B衍生物,并测试了它们的生物活性。合成该类化合物的关键中间体3,3″,6′/2′,3,3″,6′-三/四-N-特丁氧羰基(Boc)-丁胺卡那霉素(4/5)的制备。按文献方法先将二/三-N-Boc-卡那霉素 A(1a/1b)载换成二/三-N-(Boc)-单-N-苄氧羧
In the transformation of aminoglycosides, the trial of a more alkaline gene to replace the amino group to enhance the basicity of the compound, so that can improve the antibacterial activity of drugs, but not to increase the toxicity, for the synthesis of a series of 1- N- [4- (substituted) amidino / guanidino 2-hydroxybutyryl] kanamycin A and B derivatives and tested for their biological activity. The key intermediates for the synthesis of this class of compounds are 3,3 “, 6 ’/ 2’, 3,3”, 6’-tris-tetrabutanamycin (4 / 5). According to the literature method, di / tri-N-Boc-kanamycin A (1a / 1b) is first exchanged for di / tri-N-