Albrecht H A, Beskid G, Christenson J G, Durkin J W, Fallat V, Georgopapadakou N H, Keith D D, Konzelmann F M, Lipschitz E R, McGarry D H
Roche Research Center, Hoffmann-La Roche Inc., Nutley, New Jersey 07110.
J Med Chem. 1991 Feb;34(2):669-75. doi: 10.1021/jm00106a031.
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.
当头孢菌素通过与细菌酶反应发挥其生物活性时，β-内酰胺环的打开会导致3'-取代基的排出。制备了一系列头孢菌素，其中抗菌喹诺酮类通过季氮连接到3'-位。与早期报道的3'-酯连接的双作用头孢菌素一样，这些化合物表现出源自头孢菌素样和喹诺酮样成分的广谱抗菌活性，提示其具有双重作用模式。
