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

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-...

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Veröffentlicht in:	Chemical & pharmaceutical bulletin 1987/02/25, Vol.35(2), pp.642-646
Hauptverfasser:	SAKAMOTO, FUMIO, IKEDA, SHOJI, HIRAYAMA, RYOICHI, MORIYAMA, MASARU, SOTOMURA, MIKIO, TSUKAMOTO, GORO
Format:	Artikel
Sprache:	eng
Schlagworte:	(5-methyl-2-oxo-1, 3-dioxol-4-yl) methyl ester Amdinocillin - analogs & derivatives Amdinocillin - chemical synthesis Amdinocillin - metabolism Amdinocillin - pharmacology Animals Chemistry Escherichia coli - drug effects Exact sciences and technology Heterocyclic compounds Heterocyclic compounds with n hetero atom and also o and/or s, se, te hetero atoms Intestinal Absorption mecillinam ester mecillinam prodrug Mice oral absorbability Organic chemistry Preparations and properties pro-moiety Structure-Activity Relationship
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Zusammenfassung:	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.
ISSN:	0009-2363 1347-5223
DOI:	10.1248/cpb.35.642