Tsushima M, Kano Y, Umemura E, Iwamatsu K, Tamura A, Shibahara S
Pharmaceutical Research Center, Meiji Seika Kaisha, Ltd., Yokohama, Japan.
Bioorg Med Chem. 1998 Sep;6(9):1641-53. doi: 10.1016/s0968-0896(98)00103-5.
A series of cephalosporin derivatives with a thiazolopyridinium group at the 3-position was synthesized and evaluated for antibacterial activity. Some of these cephalosporin derivatives having a (5-alkylthiazolo[4,5-c]pyridinium-2-yl)thiomethyl group at the 3-position showed strong activity against Gram-positive and Gram-negative bacteria, including Pseudomonas aeruginosa. Among them, 5a showed a good antibacterial spectrum in vitro, and also showed a similar or slightly superior activity to that of ceftazidime in vivo against P. aeruginosa.
合成了一系列在3位带有噻唑并吡啶鎓基团的头孢菌素衍生物,并对其抗菌活性进行了评估。其中一些在3位带有(5-烷基噻唑并[4,5-c]吡啶鎓-2-基)硫甲基基团的头孢菌素衍生物对革兰氏阳性菌和革兰氏阴性菌表现出较强的活性,包括铜绿假单胞菌。其中,5a在体外显示出良好的抗菌谱,并且在体内对铜绿假单胞菌的活性与头孢他啶相似或略优于头孢他啶。