7-(1,7-双取代-1,4-二氢-4-酮-1,8-萘啶-3-甲酰氨基)头孢菌素的合成

本文报道了以1,7-双取代-1,4-二氢-4-酮-1,8-萘啶-3-羧酸,用混合酸酐法与7-ACA,7-ADCA,7-ACT和7-ACD缩合,合成了24个1,7-双取代-1,4-二氢-4-酮-1,8-萘啶-3-甲酰胺头孢菌素衍生物,通过葡聚糖凝胶(Sephadex LH-20)及离心薄层层析纯化精制,得到纯品。体外抑菌试验结果表明:大多数新头孢菌素衍生物对革兰氏阳性菌具有较好的抗菌作用。尚有一些新头孢菌素衍生物对某些革兰氏阴性菌具有中等敏感程度。

SYNTHESIS OF 7-(I,7-DISUBSTITUTED- 1,4-DIHYDRO-4-OXO-1,8-NAPHTHYRIDINE-3-CARBOXAMIDO)-CEPHALOSPORINS

A series of new 7-(1, 7-disubstituted-1, 4-dihydro-4-oxo-1, 8-naphthyridine-3-carboxamido)-cephalosporins has been prepared by acylation of the 7-amino group of 7-ADCA, 7-ACA, 7-ACT and 7-ACD with 1, 7-disubstituted-1, 4-dihydro-4-oxo-1,8-naphthyridine-3-carboxylic acid. Mixed carboxylic-carbonic anhydride method was adopted in the reactions. Isolation and purification were fulfilled with Sephadex LH-20 column chromatography and centrifugal-TLC technique. Twenty four new cephalosporin derivatives were synthesized. Their structures have been confirmed by elemental analysis, IR and 1HNMR. In preliminary In vitro antibacterial sensitivity tests, most of these new derivatives were found to show good sensitivity to Gram-positive bacteria. Bacteriostasis were also observed for some Gram-negative bacteria.