7β-(6-取代-2-喹诺酮-3-乙酰氨基)头孢菌素的合成

以6-取代-2-喹诺酮-3-乙酸为侧链,用CDI法和潘化酯法与7-ADCA,7-ACA,7-ACT,和7-ACD缩合,合成了16个新的7β-(6-取代-2-喹诺酮-3-乙酰氨基)头孢菌素类化合物,通过溶媒转提,葡聚糖凝胶(Sephadex LH-20)柱层析及离心薄层层析分离精制,得到纯品。初步体外抑菌试验表明:新化合物对革兰氏阳性及某些阴性菌具有高度敏感性。大多数化合物对所试试验菌的抗菌活性与头孢唑啉和青霉素G钠相当,有些比它们还强。

Synthesis of 7 beta-(6-substituted-2-quinolone-3-acetamido)cephalosporins

A series of new 7 beta-(6-substituted-2-quinolone-3-acetamido)cephalosporins has been prepared by acylation of the 7 beta-amino group of 7-ADCA, 7-ACA, 7-ACT and 7-ACD with 6-substituted-2-quinolone-3-acetic acids. CDI (N,N'-Carbonyldiimidazole) method was mainly adopted and active ester method was also employed in the reactions. Isolation and purification were fulfilled with the combined methods of Sephadex LH-20 column chromatography and centrifugal TLC technique. Sixteen new cephalosporin derivatives were synthesized. Their structures have been confirmed by elemental analysis, IR and 1HNMR. The preliminary in vitro antibacterial tests showed that these new compounds exhibited high activity to gram-positive and some negative bacteria. Bacteriostasis of most of the compounds was equal to cefazolin and sodium penicillin G. Compound III3, III4, III8, III10 and III11 possessed higher activity on the resistant Staphylococcus aureus S22 and Proteus vulgaris OX19 than cefazolin and sodium penicillin G. Further biological evaluation for these compounds is expected to be carried out.