[Synthesis of 7-(1,7-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.
Zhou
J C
JC
Duan
T H
TH
Zhou
H S
HS
D002511:Cephalosporins / Q000138:chemical synthesis* / Q000494:pharmacology; D004352:Drug Resistance, Microbial; D006094:Gram-Positive Bacteria / Q000187:drug effects; D009287:Naphthyridines / Q000138:chemical synthesis* / Q000494:pharmacology
D002511:Cephalosporins; D009287:Naphthyridines