Iwamatsu K, Atsumi K, Sakagami K, Ogino H, Yoshida T, Tsuruoka T, Shibahara S, Inouye S, Kondo S
Pharmaceutical Research Center, Meiji Seika Kaisha, Ltd., Yokohama, Japan.
J Antibiot (Tokyo). 1990 Nov;43(11):1450-63. doi: 10.7164/antibiotics.43.1450.
The synthesis and biological activity of a series of 3-[2-(5-hydroxy-4-pyridon-2-yl)ethenyl]cephalosporin derivatives are described. They showed very potent activity against Gram-negative bacteria, especially Pseudomonas aeruginosa. (6R, 7R)-7-[(Z)-2-(2-Aminothiazol-4-yl)-2 -(1-carboxy-1-methyl)-ethoxyiminoacetamido]-3-[(Z)-2-(1,5-dihydrox y-4- pyridon-2-yl)ethenyl]ceph-3-em-4-carboxylic acid, CP6162 (8e), was selected for further evaluation as antipseudomonal chemotherapeutic agent.
描述了一系列3-[2-(5-羟基-4-吡啶酮-2-基)乙烯基]头孢菌素衍生物的合成及其生物活性。它们对革兰氏阴性菌表现出非常强的活性,尤其是铜绿假单胞菌。(6R, 7R)-7-[(Z)-2-(2-氨基噻唑-4-基)-2 -(1-羧基-1-甲基) -乙氧基亚氨基乙酰氨基]-3-[(Z)-2-(1,5-二羟基-4-吡啶酮-2-基)乙烯基]头孢-3-烯-4-羧酸,CP6162 (8e),被选作抗铜绿假单胞菌化疗药物进行进一步评估。