Uri J V, Phillips L, Pitkin D H
Acta Microbiol Hung. 1986;33(2):131-40.
Eleven new cephalosporins (three phenylacetamido and eight furylacetamido) containing a methoxyimino group on the 7 beta-acyl side chain and having various substituents at their 3-positions, exhibited similar qualitative, but differing quantitative in vitro antibacterial spectra compared to that of cefuroxime, the first therapeutically used alpha-methoxyimino cephalosporin. The syn-isomers and the alpha-acyl substituted compounds are more active than either the anti-isomer or the beta-acyl substituted compounds. Compounds containing substituted tetrazole rings at the 3-position are likewise more active than those containing other types of substituents in this position. In vivo (mouse) the heterocyclic furylacetamido compounds are more efficacious (protective) than the aromatic phenylacetamido compounds. The furylacetamido alpha-methoxyimino cephalosporins containing at the 3-position the tetrazole group carrying an acidic function possess favorable pharmacokinetic properties, i.e., higher serum levels and prolonged biological half-lives in mouse and squirrel monkey and extensive binding to serum proteins.
11种新的头孢菌素（3种苯乙酰胺基和8种呋喃乙酰胺基），在其7β-酰基侧链上含有甲氧基肟基，且在3位具有不同取代基，与首个用于治疗的α-甲氧基肟头孢菌素头孢呋辛相比，呈现出相似的定性但不同的定量体外抗菌谱。顺式异构体和α-酰基取代化合物比反式异构体或β-酰基取代化合物更具活性。在3位含有取代四唑环的化合物同样比在该位置含有其他类型取代基的化合物更具活性。在体内（小鼠），杂环呋喃乙酰胺基化合物比芳香族苯乙酰胺基化合物更有效（有保护作用）。在3位含有带酸性功能的四唑基团的呋喃乙酰胺基α-甲氧基肟头孢菌素具有良好的药代动力学性质，即在小鼠和松鼠猴体内血清水平较高、生物半衰期延长，并且与血清蛋白广泛结合。
