DUAL-ACTION CEPHALOSPORINS - CEPHALOSPORIN 3'-QUATERNARY AMMONIUM QUINOLONES

被引:38
作者
ALBRECHT, HA
BESKID, G
CHRISTENSON, JG
DURKIN, JW
FALLAT, V
GEORGOPAPADAKOU, NH
KEITH, DD
KONZELMANN, FM
LIPSCHITZ, ER
MCGARRY, DH
SIEBELIST, J
WEI, CC
WEIGELE, M
YANG, R
机构
[1] Roche Research Center, Hoffmann-La Roche Inc., Nutley
关键词
D O I
10.1021/jm00106a031
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
When cephalosporins exert their biological activity by reacting with bacterial enzymes, opening of the beta-lactam ring can lead to expulsion of the 3'-substituent. A series of cephalosporins was prepared in which antibacterial quinolones were linked to the 3'-position through a quaternary nitrogen. Like the 3'-ester-linked dual-action cephalosporins reported earlier, these compounds demonstrated a broad spectrum of antibacterial activity derived from cephalosporin-like and quinolone-like components, suggesting a dual mode of action.
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页码:669 / 675
页数:7
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