頁籤選單縮合
題名 | Preparation of D-Phenylglycinyl Derivatives of Cefuroxime as Double Ester Prodrugs= |
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作者 | 李嘉帥; 宋啟華; 王惠珀; Lee, Jia-shuai; Sun, Chi-hua; Wang, Hui-po; |
期刊 | 中華藥學雜誌 |
出版日期 | 19970600 |
卷期 | 49:3 1997.06[民86.06] |
頁次 | 頁195-205 |
分類號 | 418.4 |
語文 | eng |
關鍵詞 | Cefuroxime prodrugs; D-phenylglycine; |
英文摘要 | D-Phenylglycine was attached at the 4-COOH of cefuroxime via an ethylidene linkage to from double ester derviatives 1a and 1b. The D-phenylglycine moiety was considered as a tool for delivering the poorly absorbed cefuroxime through the intestine. The △�纂驉詁� isomerization commonly reported along the preparation of cephalosporin esters was successfully eliminated by adding TBA�廈SO as phase transfer catalyst in the alkylation reaction. The prodrugs were stable in acidic phosphate buffer solutions, but degraded fairly rapidly in pH 7.39 phosphate buffer solution and in rat intestinal mucosea suspensio. The t�� for 1a and 1b were 10 min and 5 min respectively, indicating that both compounds fail to demonstrate satisfactory stability for fomulation as oral prodrugs of cefuroxime. |
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