| 摘要 |
<p>Cpds. of formula (I) and their pharmaceutically acceptable salts are new (m= 0 or 1; n= 2-5). - (I) is a broad spectrum antibiotic effective against gram-positive and gram-negative bacteria and their resistant strains. (I) is rapidly hydrolysed in vivo to give the corresp. 4-carboxylic acid (II), a known antibiotic highly effective against e.g. Staphylococcus aureus, Escherichia coli, Klebsiella pneumoniae, Proteus vulgaris, P. mirabilis and P. morganii. - (I) is well absorbed into the gastro-intestinal tract, partic. in the form of its acid addn. salts which have increased water solubility. This form of the cpd. also serves to stabilise it, facilitating both isolation of (I) and its pharmaceutical processing. The prefd. salt is the monohydrochloride or esp. the dihydrochloride. - (I) has low toxicity (LD50 at least 3 g/kg p.o. in mice). (I) is administered in 3 or 4 divided doses at 0.3-5 (pref. 0.5-3) g/day/adult. - Specifically claimed is 1-(cyclohexylacetoxy)ethyl 7beta-(2- (2-aminothiazol-4-yl) acetamido)-3-(((1-(2-dimethylamino-ethyl) -1H-tetrazol-5-yl) thio)methyl) ceph-3-em-4-carboxylate. (0/0)</p> |
