Synthesis and Oral Absorption of Hetacillin and Hetamoxicillin Labile Esters

Nine esters of hetacillin or hetamoxicillin were synthesized as ampicillin and amoxicillin derivatives with the aim of obtaining improved plasma levels after oral administration. Out of these esters, which are devoid of apparent toxic effects, the benzyloxymethyl ester of hetacillin (FI-5204) gave t...

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Published inChemical & pharmaceutical bulletin Vol. 35; no. 6; pp. 2366 - 2372
Main Authors GUBERT, SANTIAGO, PALACIN, CELIA, SACRISTÁN, AURELIO, ORTIZ, JOSÉ A.
Format Journal Article
LanguageEnglish
Published Tokyo The Pharmaceutical Society of Japan 1987
Maruzen
Japan Science and Technology Agency
Subjects
Animals
benzyloxymethyl ester
Chemistry
Esters
Exact sciences and technology
Female
hetacillin ester
Heterocyclic compounds
Heterocyclic compounds with n hetero atom and also o and/or s, se, te hetero atoms
Intestinal Absorption
Male
Mice
oral absorption
Organic chemistry
oxyhetacillin ester
Penicillins - chemical synthesis
Penicillins - pharmacokinetics
Penicillins - toxicity
plasma level
Preparations and properties
prodrug
Sulfur nitrogen heterocycle
Five membered ring
Nitrogen heterocycle
Lactam
Oral administration
Bicyclic compound
Phenols
Prodrug
Metabolism
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Summary:Nine esters of hetacillin or hetamoxicillin were synthesized as ampicillin and amoxicillin derivatives with the aim of obtaining improved plasma levels after oral administration. Out of these esters, which are devoid of apparent toxic effects, the benzyloxymethyl ester of hetacillin (FI-5204) gave the best result and was chosen for subsequent studies.
Bibliography:ObjectType-Article-2
SourceType-Scholarly Journals-1
ObjectType-Feature-1
content type line 23
ISSN:0009-2363
1347-5223
DOI:10.1248/cpb.35.2366