Studies on Penem and Carbapenem. I. : Syntheses and Oral Absorption of Ester-Type Prodrugs of Sodium (5R, 6S)-2-(2-Fluroethylthio)-6-[(1R)-1-hydroxyethyl]penem-3-carboxylate

概要

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Acyloxyalkyl esters (2a-d), alkyloxycarbonyloxyalkyl esters (2e-g) and (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl ester (2h) of (5R, 6S)-2-(2-fluoroethylthio)-6-[(1R)-1-hydroxyethyl]penem-3-carboxylic acid (1) were synthesized. Enhanced oral absorption was observed in mice reflecting increased lipophilicity, compared with the parent 1 itself. Among them, the ester 2h showed a prolonged plasma level and a large area under the blood concentratino-time curve (AUC) in rats. These ester-type prodrugs of penem 1 in phosphate buffer (pH 6.86) were much more stable than those of cephalosporins which easily degraded via isomerization to Δ^2 cephalosporins.
社団法人日本薬学会の論文
1990-06-25