Hikida M, Inoue M, Mitsuhashi S
J Antimicrob Chemother. 1986 Nov;18(5):585-91. doi: 10.1093/jac/18.5.585.
L-105 (sodium(-)-(6R, 7R)-7-[(Z)-2-(2-amino-4-thiazolyl)-2-methoxyimino- acetamido]-3-[1,2,3-thiadiazol-5-yl)thiomethyl]-8-oxo-5-thia-1-aza bicyclo [4.2.0]oct-2-ene-2-carboxylate) is a new semisynthetic cephalosporin derivative. The in-vitro antibacterial activity of L-105 against clinical isolates of 18 bacterial species was compared with those of cefmenoxime, cefoperazone and cefazolin. Its spectrum against Gram-negative bacteria was similar to that of cefmenoxime. Moreover, against Gram-positive bacteria, including Staphylococcus aureus, coagulase negative staphylococci, Streptococcus faecalis, Str. pneumoniae and Str. pyogenes, L-105 was more potent than cefmenoxime and cefoperazone. Against Gram-positive bacteria, including Staph. aureus which is comparatively resistant to most third-generation cephalosporins, it was nearly equal in potency to cefazolin. L-105 was stable to various penicillinases and cephalosporinases. However, this compound was slightly hydrolyzed by oxyiminocephalosporinases, i.e., the enzymes produced by Pseudomonas cepacia and Ps. maltophilia.
L - 105((6R,7R)-7 - [(Z)-2 - (2 - 氨基 - 4 - 噻唑基)-2 - 甲氧基亚氨基乙酰胺基]-3 - [1,2,3 - 噻二唑 - 5 - 基)硫甲基]-8 - 氧代 - 5 - 硫杂 - 1 - 氮杂双环[4.2.0]辛 - 2 - 烯 - 2 - 羧酸钠)是一种新型半合成头孢菌素衍生物。将L - 105对18种细菌临床分离株的体外抗菌活性与头孢甲肟、头孢哌酮和头孢唑林进行了比较。其对革兰氏阴性菌的抗菌谱与头孢甲肟相似。此外,对于革兰氏阳性菌,包括金黄色葡萄球菌(金葡菌)、凝固酶阴性葡萄球菌、粪肠球菌、肺炎链球菌和化脓性链球菌,L - 105比头孢甲肟和头孢哌酮的抗菌活性更强。对于革兰氏阳性菌,包括对大多数第三代头孢菌素相对耐药的金葡菌,其抗菌活性与头孢唑林相近。L - 105对各种青霉素酶和头孢菌素酶稳定。然而,该化合物会被氧亚氨基头孢菌素酶轻微水解,即洋葱伯克霍尔德菌和嗜麦芽窄食单胞菌产生的酶。