Valcavi U, Brandt A, Corsi G B, Innocenti S, Minoja F, Pascucci G
Farmaco Sci. 1980 Jul;35(7):563-72.
The antibacterial activity of some ureido, acylureido and carbamoylureido derivatives of cephalexin and cefadroxil, prepared in our laboratories, as compared to parent compounds is reported. Only the 7-[D-alpha-(imidazolidin-2-one-1-ylcarbonylamino)-alpha-phenylacetamido]-3-methyl-3-cephem-4-carboxylic acid (IV d) and the 7-[D-alpha-(imidazolidin-2-one-1-ylcarbonylamino)-alpha-p-hydroxyphenylacetamido]-3-methyl-3-cephem-4-carboxylic acid (V c) showed some antibiotic activity. However we found no activity improvement against Pseudomonas strains (contrary to the results obtained in similar penicillin derivatives) and a lower beta-lactamase resistance.
据报道,我们实验室制备的头孢氨苄和头孢羟氨苄的一些脲基、酰脲基和氨基甲酰脲基衍生物与母体化合物相比的抗菌活性。只有7-[D-α-(咪唑烷-2-酮-1-基羰基氨基)-α-苯乙酰胺基]-3-甲基-3-头孢烯-4-羧酸(IV d)和7-[D-α-(咪唑烷-2-酮-1-基羰基氨基)-α-对羟基苯乙酰胺基]-3-甲基-3-头孢烯-4-羧酸(V c)表现出一些抗生素活性。然而,我们发现对假单胞菌菌株没有活性提高(与在类似青霉素衍生物中获得的结果相反),并且β-内酰胺酶抗性较低。