Yamanaka H, Kawabata K, Miyai K, Takasugi H, Kamimura T, Mine Y, Takaya T
J Antibiot (Tokyo). 1986 Jan;39(1):101-10. doi: 10.7164/antibiotics.39.101.
The synthesis of 7 beta-([Z) -2-(2-amino-4-thiazolyl)-2-(carboxymethoxyimino) acetamido]-cephalosporins (2a-h) modified at the C-3 position of a cephem nucleus and the effect of the C-3 substituents on the antibacterial activity, oral absorptivity and therapeutic activity are discussed. The cephems (2a and 2b) having a C-3 substituent such as hydrogen or vinyl were more potent than other cephalosporins against Gram-negative bacteria. However, the cephalosporin (2f) having methylthio group at the 3-position showed the highest absorption rate in rats. These three cephalosporins (2a, b and f) exhibited equally good protective activities in mice infected. Furthermore, the serum levels of these cephalosporins (2a, b and f) were examined in dogs, and 2b and 2f showed outstanding high and prolonged serum levels.
讨论了在头孢烯核的C-3位修饰的7β-([Z)-2-(2-氨基-4-噻唑基)-2-(羧基甲氧基亚氨基)乙酰胺基]-头孢菌素(2a-h)以及C-3取代基对抗菌活性、口服吸收性和治疗活性的影响。具有氢或乙烯基等C-3取代基的头孢烯(2a和2b)对革兰氏阴性菌的活性比其他头孢菌素更强。然而，在3位具有甲硫基的头孢菌素(2f)在大鼠中显示出最高的吸收率。这三种头孢菌素(2a、b和f)在感染小鼠中表现出同样良好的保护活性。此外，在犬中检测了这些头孢菌素(2a、b和f)的血清水平，2b和2f显示出极高且持久的血清水平。
