【摘要】 本文报告了C₃次甲基含氮杂环取代的7-脒硫乙酰胺基头孢菌素衍生物的合成,比较了化学结构与抗菌活性之间的关系,发现化合物C-7905、C-7906、C-7907,C-7908,C-7910、C-7911和C-7924等的抗菌活性较好,对革兰氏阴性菌的作用优于硫脒头孢菌素,其中C-7906、C-7907、C-7911和C-7924尤为突出,其抗菌活性接近唑啉头孢菌素。更多还原

【Abstract】 Although cefathiamidine, one of the new semisynthetic antibiotics, has been used favorably in clinics, it is not efficacious enough for the control of gram-negative organisms. In order to find derivatives more active than the parent substance a series of new compounds, containing the substituted amidinothio group in the side chain at the C-7 position of cephalosporin and different heterocycles at the C-3 methylene position, has been synthesized. After preliminary screening it was found that compounds C-7906, C-7907, C-7911 and C-7924 showed high activity against gram-negative organisms as well as gram-positive organisms. Their activities are comparable with those of cefazolin.更多还原