7-[(1S,4S)-3,3-二甲基-2-氧杂-5-氮杂二环[2.2.1]庚烷-5-基]-喹诺酮化合物的合成与抗菌作用

Synthesis and Antibacterial Activity of 7-[(1S,4S)-3,3-Dimethyl-2-oxa-5-azabicyclo[2.2.1] heptane-5-yl] quinolones

以 (4R) -羟基 - L-脯氨酸为起始原料 ,经 8步反应合成了 (1S,4 S) - 3,3-二甲基 - 2 -氧杂 - 5 -氮杂二环 [2 .2 .1]庚烷 ,以此化合物作为喹诺酮类的 7-位侧链 ,合成了 3个衍生物 ,并测定了它们对 10株革兰阳性菌和 6株革兰阴性菌的 MIC值。结果表明 ,它们的体外抗菌活性均低于对照药加替沙星和环丙沙星。

S,4S) 3,3 Dimethyl 2 oxa 5 azabicyclo[2.2.1] heptane was synthesized by 8 steps from trans 4 hydroxy L proline. Three quinolone derivatives were synthesized with this compound as the side chain at position 7 and their MIC against 16 clinical isolates were detected. The result showed that they had very low antibacterial activities compared to ciprofloxacin and gatifloxacin.