口服活性头孢菌素酯的研究。VI. 3-(3-异恶唑基)氧甲基头孢菌素衍生物的合成及抗菌活性
Studies on orally active cephalosporin esters. VI. Synthesis and antimicrobial activity of 3-(3-isoxazolyl)oxymethylcephalosporin derivatives.
作者信息
Nakayama E, Watanabe K, Miyauchi M, Fujimoto K, Ide J
机构信息
Sankyo Research Laboratories, Sankyo Co., Ltd., Tokyo, Japan.
出版信息
J Antibiot (Tokyo). 1990 Sep;43(9):1122-30. doi: 10.7164/antibiotics.43.1122.
The synthesis and biological activities of a series of 3-(isoxazol-3-yl)oxymethyl cephalosporins are described. 7-[2-(2-Aminothiazol-4-yl)-(Z)-2-methoxyiminoacetamido]-3- [(isoxazol-3-yl)oxymethyl]-3-cephem-4-carboxylic acid (7a) showed potent activity against both Gram-positive and Gram-negative bacteria including some beta-lactamase producing species. Its pivaloyloxymethyl ester provided a good urinary recovery after oral administration to mice.
描述了一系列3-(异恶唑-3-基)氧甲基头孢菌素的合成及其生物活性。7-[2-(2-氨基噻唑-4-基)-(Z)-2-甲氧基亚氨基乙酰胺基]-3-[(异恶唑-3-基)氧甲基]-3-头孢烯-4-羧酸（7a）对革兰氏阳性菌和革兰氏阴性菌均显示出强效活性，包括一些产β-内酰胺酶的菌株。其新戊酰氧甲基酯经小鼠口服给药后在尿液中的回收率良好。
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