Studies on Prodrugs. VI. Preparation and Characterization of (5-Substituted 2-Oxo-1, 3-dioxol-4-yl) methyl Esters of Mecillinam

FUMIO SAKAMOTO; SHOJI IKEDA; RYOICHI HIRAYAMA; MASARU MORIYAMA; MIKIO SOTOMURA; GORO TSUKAMOTO

doi:10.1248/cpb.35.642

FUMIO SAKAMOTO, SHOJI IKEDA, RYOICHI HIRAYAMA, MASARU MORIYAMA, MIKIO SOTOMURA, GORO TSUKAMOTO

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Keywords: (5-methyl-2-oxo-1, 3-dioxol-4-yl) methyl ester, mecillinam prodrug, oral absorbability, pro-moiety, mecillinam ester

JOURNAL FREE ACCESS

1987 Volume 35 Issue 2 Pages 642-646

DOI https://doi.org/10.1248/cpb.35.642

[Correction] Chem. Pharm. Bull. Vol.35 No.6 (1987) pp.2622c-2622c

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Abstract

As a new type of mecillinam prodrug, mecillinam (5-substituted 2-oxo-1, 3-dioxol-4-yl) methyl esters were prepared. These esters were found to produce at least 4-fold higher mecillinam levels in blood than mecillinam itself after oral administration to mice. Mecillinam (5-methyl-2-oxo-1, 3-dioxol-4-yl) methyl ester hydrochloride was hygroscopic, but its L-tartrate was not.

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