半合成头孢菌素。7-(1-吡咯基)-和7-(1-吲哚基)乙酰胺基头孢菌素衍生物的合成及构效关系
Semisynthetic cephalosporins. Synthesis and structure-activity relationships of 7-(1-pyrryl)- and 7-(1-indolyl)acetamidocephalosporin derivatives.
作者信息
Nudelman A, Karoly H, Braun F, Böhme E H, Erickson R C
出版信息
J Med Chem. 1978 Sep;21(9):962-4. doi: 10.1021/jm00207a022.
A series of 1-pyrrole- and 1-indoleacetamido derivatives of 3-heteroaryl-substituted cephalosporins was prepared. The most active compound in the series was 7-[[2-(1-pyrryl)acetyl]amino]-3-[[(1-methyltetrazol-5-yl)thio]-methyl]-8-oxo-5-thia-1-azabicyclo[4.2.0]oct-2-ene-2-carboxylic acid (6), which showed comparable potency in vitro and in vivo to that of cefazolin, and, in addition, was more potent than cefazolin against Enterobacter sp. and Providencia stuartii.
制备了一系列3-杂芳基取代头孢菌素的1-吡咯和1-吲哚乙酰胺衍生物。该系列中活性最高的化合物是7-[[2-(1-吡咯基)乙酰基]氨基]-3-[[(1-甲基四氮唑-5-基)硫代]甲基]-8-氧代-5-硫杂-1-氮杂双环[4.2.0]辛-2-烯-2-羧酸（6），其在体外和体内显示出与头孢唑林相当的效力，此外，对肠杆菌属和斯氏普罗威登斯菌的效力比头孢唑林更强。
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