セファロスポリンPro-drugに関する研究 : (5-Methyl-2-oxo-1,3-dioxol-4-yl)methyl 7-[D-O-(Aminoacyl)mandelamido]-3-[[(5-methyl-1,3,4-thiadiazol-2-yl)thio]methyl]-3-cephem-4-carboxylate類の合成, 経口吸収及び抗菌活性

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Bifunctional pro-drugs of 7-(D-mandelamido)-3[[(5-methyl-1,3,4-thiadiazol-2-yl)thio]-methyl]-3-cephem-4-carboxylic acid (KY-087), incorporating both lipophilic and hydrophilic pro-moieties, were designed to improve the oral absorption of KY-087,a cephalospolin with a broad spectrum of antibacterial activity. The synthesized pro-drugs were found to possess a sufficient aqueous solubility and an optimal lability. The pro-drugs were evaluated for the oral absorption in mice. Among the pro-drugs tested, KY-109 carring a (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl (DOX) pro-moiety and an L-alanyl pro-moiety was particularly well absorbed orally and, as expected, displayed good antibacterial activity in the experimental infection in mice.
社団法人日本薬学会の論文
1988-08-25