| 摘要 |
Disclosed are substituted N-methylene derivatives of thienamycin having the formula: <IMAGE> wherein: (1.) X=-NR1R2, and Y=-R'-N=CRNR1R2, and (2.) X=R, and Y=-NR1R'N=CRNR1R2; and wherein: R is, inter alia, hydrogen, NH2, -NHR1, -NR1R2, R1 and R2; R1 and R2 are independently selected from: hydrogen, substituted, or unsubstituted: alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aryl, aralkyl, heteroaryl, heteroaralkyl, heterocyclyl, and heterocyclylalkyl; R' is -(CH2)n-, n is 1-6, or -(CH2)m-Q-(CH2)p-, m, n=1-3 and Q is O, S or R' is a carbocyclic or heterocyclic ring. Such compounds and their pharmaceutically acceptable salt, ether, ester and amide derivatives are useful as antibiotics. Also disclosed are processes for the preparation of such compounds, pharmaceutical compositions comprising such compounds; and methods of treatment comprising administering such compounds and compositions when an antibiotic effect is indicated.
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