6-[.alpha.-(Imidazolidin-2-on-1-ylcarbonylamino)-substutited acetamido]penicillanic acids, and the correspondingly 7-substituted ceph-3-em-4-carboxylic acids, characterized by the presence of a methyleneamino or substituted methyleneamino group on the 3-nitrogen atom of the imidazolidine ring are antibacterial agents. The compounds, of which 6-[.alpha.-(3-benzaliminoimidazolidin-2-on-1-ylcarbonylamino)cyclohe xa-1,4-dien-1-ylacetamido]penicillanic acid and 7-[.alpha.-(3-furylideneaminoimidazolidin-2-on-1-ylcarbonylamino)phenylace tamido]-3-(3-methylthiadiazol-5-ylthiomethyl)ceph-3-em-4-carboxylic acid are typical examples, are prepared through acylation of an 6-[.alpha.-(amino)substituted acetamido]penicillanic acid or the corresponding 7-[.alpha.-(amino)substituted acetamido]ceph-3-em-4-carboxylic acid with a reactive nucleofugic derivative of a 3-methyleneaminoimidazolidin-2-on-1-carboxylic acid.
6-[.alpha.-(
咪唑啉-2-酮-1-基甲酰
氨基)-取代乙酰胺基]青霉烷酸和相应的7-取代头孢-3-酮-4-
羧酸,其特征在于
咪唑啉环的3-氮原子上存在甲
亚胺基或取代甲
亚胺基,是抗菌剂。这些化合物,例如6-[.alpha.-(3-苯甲
酰亚胺基
咪唑啉-2-酮-1-基甲酰
氨基)环己-1,4-二烯-1-乙酰胺基]青霉烷酸和7-[.alpha.-(3-
呋喃亚烯基
氨基
咪唑啉-2-酮-1-基甲酰
氨基)苯乙酰胺基]-3-(3-甲基
噻二唑-5-基
硫甲基)头孢-3-酮-4-
羧酸是典型的例子,是通过用3-甲
亚胺基
咪唑啉-2-酮-1-
羧酸的反应性亲核衍
生物对6-[.alpha.-(
氨基)取代乙酰胺基]青霉烷酸或相应的7-[.alpha.-(
氨基)取代乙酰胺基]头孢-3-酮-4-
羧酸进行酰化制备的。