Vinylthioacetamido oxacephalosporin derivatives, and intermediates therefor, their preparation, formulations containing the same and their antibacterial use
申请人:SHIONOGI & CO., LTD.
公开号:EP0107928A1
公开(公告)日:1984-05-09
A compound of the formula:
wherein A is hydroxy or a group of the formula:
in which u represents hydrogen, carboxamido, N-hydroxy- carboxamido, carboxy, azido, aryl, acylamino, protected carboxy or N-alkoxycarboxamido, or, together with v, represents -S- or -CH2S-; v represents hydrogen, halogen, cyano or alkylthio, or, together with u, represents -S- or -CH2S-, or, together with w, represent -(CH2)3CO-; w represents hydrogen, carbamoyl, cyano, carboxy, N-alkylcarbamoyl, alkyl, aryl protected carboxy or a heterocycle group, or, together with v, represents -(CH2)3CO-; x represents halogen, trifluoromethyl, alkylthio or arylthio; y represents hydrogen, a light metal or a carboxylic acid-protecting group; and z represents acyloxy or a heterecycle-thio group; each of u, v, w, x, y and z being optionally substituted by halogen or a carbon-, nitrogen-, oxygen- or sulfur-containing functional group; or a derivative of said compound in which A is hydroxy. Such compounds are useful as antibacterial compounds or as intermediates therefor.
式的化合物:
其中 A 是羟基或式中的基团:
其中 u 代表氢、羧酰胺基、N-羟基-羧酰胺基、羧基、叠氮基、芳基、酰氨基、受保护的羧基或 N-烷氧基羧酰胺基,或与 v 一起代表-S-或-CH2S-;v 代表氢、卤素、氰基或烷硫基,或与 u 一起代表-S- 或-CH2S-,或与 w 一起代表-(CH2)3CO-; w 代表氢、氨基甲酰基、氰基、羧基、N-烷基氨基甲酰基、烷基、芳基受保护羧基或杂环基团,或与 v 一起代表-(CH2)3CO-;x代表卤素、三氟甲基、烷硫基或芳硫基;y代表氢、轻金属或羧酸保护基团;z代表酰氧基或杂环硫基;u、v、w、x、y和z中的每一个可任选地被卤素或含碳、氮、氧或硫的官能团取代;或上述化合物的衍生物,其中A为羟基。此类化合物可用作抗菌化合物或其中间体。