Synthesis and biological activity of 7 beta-(2-amino-2-carboxy)-ethylthioacetamido-7 alpha-methoxycephalosporin derivatives.
Synthesis and biological activity of 7 beta-(2-amino-2-carboxy)-ethylthioacetamido-7 alpha-methoxycephalosporin derivatives.
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7β-(2-氨基-2-羧基)-乙基硫代乙酰氨基-7α-甲氧基头孢菌素衍生物的合成和生物活性。
DOI：
10.7164/antibiotics.36.229
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发表时间：
1983
期刊：
影响因子：
--
通讯作者：
T. Niida
中科院分区：
文献类型：
--
作者：
K. Iwamatsu;S. Inouye;T. Tsuruoka;K. Mizutani;S. Omoto;H. Ogino;K. Miyauchi;T. Watanabe;T. Niida
对新抗生素SF-1623的C-7和C-3位取代基进行化学修饰以提高其生物活性，并根据对选定细菌的MIC和ED_（50）值考察了C-7和C-3位取代基的效应。在众多的衍生物中，MT-141的C-7位含有2-D-2-氨基-2-羧乙基硫代乙酰胺基，C-3位含有N-甲基四唑基硫甲基，在体外尤其是体内表现出较高的抗菌活性。
C-7 and C-3 substituents of a new antibiotic SF-1623 were chemically modified to improve the bioactivity, and substituent effect at C-7 and C-3 was examined on the basis of MIC and ED50 values against selected bacteria. Among a large number of derivatives, MT-141 possessing 2-D-2-amino-2-carboxyethylthioacetamido residue at C-7 and N-methyltetrazolyl-thiomethyl residue at C-3 showed a high order of antibacterial activity in vitro and especially in vivo.