摘要
分别以N-叔丁氧羰基-L-亮氨酸(L-缬氨酸)和妥舒沙星盐酸盐为原料,经缩合后在盐酸中水解得到含有L-亮氨酰基或L-缬氨酰基的2种妥舒沙星前药的盐酸盐(1a,b)。测定了它们及对照药对小鼠腹腔感染不同细菌的体内保护疗效,结果表明,1b对肺炎链球菌9798和金葡球菌15的体内活性均弱于对甲苯磺酸妥舒沙星(TSFX·TosOH);1a对肺炎链球菌9798、金葡球菌15和金葡球菌01193的体内活性均强于TSFX·TosOH。1a具有潜在的开发价值,值得进一步深入评价。
Two prodrug hydrochlorides of tosufloxacin were synthesized via condensation of tosufloxacin hydrochloride and BocAA and then hydrolyzed in hydrochloric acid. The results showed that the in vivo activity against Streptococcus pneumoniae 9798 and Staphylococcus aureus 15 of 1b is lower than TSFX·TosOH and the in vivo activity against S.pneumoniae 9798 and S.aureus 15 and S.aureus 01193 of 1a is higher than TSFX·TosOH. 1a has some potential to be studied and developed further.
出处
《中国抗生素杂志》
CAS
CSCD
北大核心
2004年第10期590-591,597,共3页
Chinese Journal of Antibiotics
关键词
氟喹诺酮
妥舒沙星前药
合成
体内活性
Fluoroquinolone
Tosufloxacin prodrugs
Synthesis
Activity in vivo
