| 摘要 |
Antibacterial 1-oxadethiacephalosporins of the formula: <IMAGE> wherein Ar is <IMAGE> <IMAGE> (in which Acyl is organic or inorganic acyl); COB1 and COB2 each is carboxy or protected carboxy; Het is <IMAGE> (in which COB3 is carboxy or protected carboxy); and Y is hydrogen or methoxy; and when COB1 and COB2, and/or COB3 is carboxy, pharmaceutically acceptable salts thereof are included, but with a proviso that when Y is methoxy, Het is <IMAGE> a pharmaceutical or veterinary composition comprising the said 1-oxadethiacephalosporins and pharmaceutical carrier, and a method for treating or preventing human or veterinary infectious diseases comprising administering the said 1-oxadethiacephalosporin. Also disclosed are epimers of the compounds of formula (I) wherein the asymmetric carbon of the malonic methine is in the D(R)- or L(S)- configuration. The individual epimers are separable by column chromatography and/or crystallization. The bactericidal activity of the D-epimers is greater than that of the L-epimers or the mixtures of the epimers. |
