📜6-氯咪唑并[1,2-B]哒嗪置于ammonium Hydroxide体系中,化学反应 8.0H,以85%的收率获得产物咪唑并[1,2-B]哒嗪-6-胺
参考文献:Studies On Anti-Mrsa Parenteral Cephalosporins. I. Synthesis And Antibacterial Activity Of 7.Beta.-[2-(5-Amino-1,2,4-Thiadiazol-3-yl)-2(Z)-Hydroxyiminoacetamido]-3-(Substituted Imidazo [1,2-B]-Pyridazinium-1-yl)Methyl-3-Cephem-4-Carboxylates And Related Compounds.
标题:Studies On Anti-Mrsa Parenteral Cephalosporins. I. Synthesis And Antibacterial Activity Of 7.Beta.-[2-(5-Amino-1,2,4-Thiadiazol-3-yl)-2(Z)-Hydroxyiminoacetamido]-3-(Substituted Imidazo [1,2-B]-Pyridazinium-1-yl)Methyl-3-Cephem-4-Carboxylates And Related Compounds.
摘要:为了提高cefozopran (Czop) 对耐甲氧西林金黄色葡萄球菌 (Mrsa) 的抗菌活性,我们开始了化学修饰,引入一个2-(5-氨基-1,2,4-噻二唑-3-基)-2(Z)-羟亚氨基乙酰基团在c-7位,以及一个3位或6位取代的咪唑[1,2-B]吡啶鎓或5位取代的咪唑[1,2-A]吡啶鎓基团在c-3'位.尽管这种方法成功地将czop对mrsa的抗性提高了两到八倍,但对包括铜绿假单胞菌在内的革兰氏阴性菌的活性略有下降.在这些新衍生物中,3-(6-氨基咪唑[1,2-B]吡啶鎓-1-基)甲基-7β-[2-(5-氨基-1,2,4-噻二唑-3-基)-2(Z)-羟亚氨基乙酰氨基]-3-头孢烯-4-羧酸酯(44A)表现出了对mrsa和革兰氏阴性菌的活性之间的非常好平衡.
DOI:10.7164/antibiotics.53.1053