3-（异恶唑啉-5-基）和3-（异恶唑-4-基）头孢菌素的合成与活性
Synthesis and activity of 3-(isoxazolin-5-yl)- and 3-(isoxazol-4-yl)cephalosporins.
作者信息
Koyama Y, Huang S P, Ikeda D, Kondo S, Takeuchi T
机构信息
Institute of Microbial Chemistry, Tokyo, Japan.
出版信息
J Antibiot (Tokyo). 1992 Dec;45(12):1930-8. doi: 10.7164/antibiotics.45.1930.
PMID:1490886
Abstract
The 1,3-dipolar cycloaddition of nitrile oxide with 3-vinylcephalosporin provided diastereomeric isomers of 3-(isoxazolin-5-yl)cephalosporin. Cycloaddition of nitrile oxide with 3-(dimethylamino-vinyl)cephalosporin gave 3-(isoxazol-4-yl)cephalosporin. These semisynthetic cephalosporins with an aminothiazole in the C-7 side chain showed moderate antibacterial activities.
摘要
腈氧化物与3-乙烯基头孢菌素的1,3-偶极环加成反应生成了3-(异恶唑啉-5-基)头孢菌素的非对映异构体。腈氧化物与3-(二甲氨基乙烯基)头孢菌素的环加成反应生成了3-(异恶唑-4-基)头孢菌素。这些在C-7侧链带有氨基噻唑的半合成头孢菌素表现出中等抗菌活性。
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