含苯并恶唑酮环的新型头孢菌素衍生物的合成及体外活性
Synthesis and in vitro activity of new cephalosporin derivatives containing a benzoxazolone ring.
作者信息
Kalcheva V, Mincheva Z, Andreeva P
机构信息
Department of Chemistry, University of Sofia, Bulgaria.
出版信息
Arzneimittelforschung. 1990 Sep;40(9):1030-4.
New cephalosporin derivatives containing a benzoxazolone ring in the side acylamino chain are synthesized using chlorides of non-substituted and halogen substituted (2-benzoxazolone-3-yl) acetic acids for the acylation of the 7-aminodesacetoxy-cephalosporanic acid and 7-amino-cephalosporanic acid amino group. Some of these new compounds exhibit a biological activity higher than that of cephalexin and cephazolin against clinical strains of Staphylococcus aureus, Staphylococcus epidermidis and Streptococcus group A and B.
使用未取代的和卤素取代的（2-苯并恶唑酮-3-基）乙酸的氯化物对7-氨基去乙酰氧基头孢烷酸和7-氨基头孢烷酸的氨基进行酰化反应，合成了侧链酰氨基链中含有苯并恶唑酮环的新型头孢菌素衍生物。其中一些新化合物对金黄色葡萄球菌、表皮葡萄球菌以及A组和B组链球菌的临床菌株表现出比头孢氨苄和头孢唑林更高的生物活性。
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