Shibahara S, Okonogi T, Yoshida T, Murai Y, Kudo T, Inouye S, Kondo S
Pharmaceutical Research Center, Meiji Seika Kaisha, Ltd., Yokohama, Japan.
J Antibiot (Tokyo). 1990 Jan;43(1):62-9. doi: 10.7164/antibiotics.43.62.
Aminothiazolylacetamidocephalosporins having 1-carboxyethoxyimino groups were synthesized and found to have excellent antibacterial activities including anti-pseudomonal activity and low toxicities. Among these cephalosporins, ME1228 having (S)-1-carboxyethoxyimino substituent and being combined with an (N-ethyl-4-pyridinio)thiomethyl group at C-3 showed marked therapeutic effects against systemic infections in mice and was selected as the best candidate for further evaluation.
合成了具有1-羧基乙氧基亚氨基的氨噻唑基乙酰胺头孢菌素，发现它们具有优异的抗菌活性，包括抗假单胞菌活性且毒性低。在这些头孢菌素中，具有（S）-1-羧基乙氧基亚氨基取代基且在C-3位与（N-乙基-4-吡啶基）硫代甲基结合的ME1228对小鼠全身感染显示出显著的治疗效果，并被选为进一步评估的最佳候选药物。
