Sakagami K, Atsumi K, Yoshida T, Nishihata K
Yakugaku Zasshi. 1989 Jun;109(6):377-87. doi: 10.1248/yakushi1947.109.6_377.
Synthesis and antibacterial activity of 7-[2-(2-aminothiazol-4-yl)-3-carboxy-2-propenoamido]cepha los porins and their derivatives are described. These compounds are of interest as carbon analogues of oximecephalosporins, 7-[2-(2-aminothiazol-4-yl)-2(Z)-oxyiminoacetamido]cephalo spo rins having remarkable antibacterial activity. The synthesized 7-[2-(2-aminothiazol-4-yl)-3(Z)-carboxy-2-propenoamido]-c eph alosporins (14, 19) show improved activity especially against the beta-lactamase-producing strains. A 7-[2-(2-aminothiazol-4-yl) maleimido]cephalosporin (15) has been also prepared by cyclization of 7-[3-(2-aminothiazol-4-yl)-2-ethoxycarbonyl-2(Z)-propenoamido++ +]cephalosporin.
描述了7-[2-(2-氨基噻唑-4-基)-3-羧基-2-丙烯酰胺基]头孢菌素及其衍生物的合成与抗菌活性。这些化合物作为肟头孢菌素的碳类似物而备受关注，肟头孢菌素7-[2-(2-氨基噻唑-4-基)-2(Z)-氧亚氨基乙酰胺基]头孢菌素具有显著的抗菌活性。合成的7-[2-(2-氨基噻唑-4-基)-3(Z)-羧基-2-丙烯酰胺基]头孢菌素（14、19）显示出改善的活性，尤其是对产β-内酰胺酶的菌株。还通过7-[3-(2-氨基噻唑-4-基)-2-乙氧羰基-2(Z)-丙烯酰胺基++]头孢菌素的环化反应制备了一种7-[2-(2-氨基噻唑-4-基)马来酰亚胺]头孢菌素（15）。
