Branch C L, Adams R G, Brain E G, Guest A W, Harrington F P, Knott S J, Pearson M J, Zomaya I I
SmithKline Beecham Pharmaceuticals, Betchworth, Surrey, U.K.
J Antibiot (Tokyo). 1993 Aug;46(8):1289-99. doi: 10.7164/antibiotics.46.1289.
The synthesis and antibacterial activity of a series of beta-lactamase stable, broad spectrum 7-[2-(2-amino-thiazol-4-yl)-2-(Z)-(methoxyimino)acetamido]-cephalo sporins, characterised by a C-3-[N-(substituted-amino)pyridinium-4-thiomethyl] group, is described. Gram-positive and Gram-negative bacteria including extended spectrum beta-lactamase-producing strains were most susceptible to the N-amino- and N-methylamino derivatives (3a) and (3b); with the exception of Pseudomonas aeruginosa, (3b) was more active in vitro and in vivo than cefpirome or ceftazidime.
描述了一系列具有β-内酰胺酶稳定性的广谱7-[2-(2-氨基噻唑-4-基)-2-(Z)-(甲氧基亚氨基)乙酰胺基]-头孢菌素的合成及抗菌活性,其特征为具有C-3-[N-(取代氨基)吡啶鎓-4-硫甲基]基团。包括产超广谱β-内酰胺酶菌株在内的革兰氏阳性菌和革兰氏阴性菌对N-氨基和N-甲基氨基衍生物(3a)和(3b)最为敏感;除铜绿假单胞菌外,(3b)在体外和体内均比头孢匹罗或头孢他啶更具活性。