Yamashita H, Minami N, Sakakibara K, Kobayashi S, Ohno M, Hamada M, Umezawa H
Department of Chemistry, Teikoku Hormone Mfg. Co., Ltd., Kanagawa, Japan.
J Antibiot (Tokyo). 1987 Dec;40(12):1716-32. doi: 10.7164/antibiotics.40.1716.
The synthesis and antibacterial activity of sodium (3S,4R)-3-[2-(2-aminothiazol-4-yl)-(Z)-2-(O-substituted oxyimino)acetamido]-2-azetidinone-1-sulfonates having various substituted ethyl groups at the C-4 position are described. Among various substituents explored, the (substituted isothiuronio)ethyl groups were found to have strong antibacterial activity against a variety of Gram-negative bacteria, and moreover, the ethylene isothiuronium derivative exhibited moderate antibacterial activity against Staphylococcus aureus.
描述了在C-4位具有各种取代乙基的(3S,4R)-3-[2-(2-氨基噻唑-4-基)-(Z)-2-(O-取代氧亚氨基)乙酰胺基]-2-氮杂环丁酮-1-磺酸钠的合成及抗菌活性。在探索的各种取代基中，发现(取代异硫脲鎓)乙基对多种革兰氏阴性菌具有很强的抗菌活性，此外，乙烯异硫脲衍生物对金黄色葡萄球菌表现出中等抗菌活性。
