[Synthesis and antimicrobial activity of 7-acylamido-3-1, 2, 3-triazol-1-ylmethyl) cephalosporins].
Yao Xue Xue Bao
; 26(3): 175-82, 1991.
Article
en Zh
| MEDLINE
| ID: mdl-1957657
ABSTRACT
In order to develop oral cephalosporin exhibiting broad-spectrum activity, a series of cephalosporin derivatives (VIII1-12) bearing 1, 2, 3-triazolymethyl substituents on the C3 position were synthesized. 7-Phenylacetamido-3-methyl-3-cephem-4-carboxylic acid (I) was employed as starting material and converted to VIII by procedures of esterification and oxidation, bromination, azido-substitution, dipolarcycloaddition, deprotection, cleavage, and condensation. Minimum inhibitory concentration (MIC) values in vitro showed that VIII2-4.9-11 had a wide antibacterial spectrum against Gram positive and Gram negative bacteria and possessed high activities. Further biological evaluation and the study of oral absorption for the six compounds will be performed.
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Banco de datos:
MEDLINE
Asunto principal:
Cefalosporinas
Idioma:
Zh
Año:
1991
Tipo del documento:
Article