STUDIES ON ORALLY ACTIVE CEPHALOSPORIN ESTERS

The synthesis and the biological properties of orally active cephalosporin esters are described. 3-Methoxymethyl cephem derivatives having a 2-(2-aminothiazol-4-yl)-(Z)-2-methoxyiminoacetamide function at C-7 (1) showed good activity against a wide variety of bacteria including some β-lactamase prod...

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Bibliographic Details
Published inJournal of antibiotics Vol. 40; no. 3; pp. 370 - 384
Main Authors FUJIMOTO, KOICHI, ISHIHARA, SADAO, YANAGISAWA, HIROAKI, IDE, JUNYA, NAKAYAMA, EJJI, NAKAO, HIDEO, SUGAWARA, SHIN-ICHI, IWATA, MASAYUKI
Format Journal Article
LanguageEnglish
Published Tokyo JAPAN ANTIBIOTICS RESEARCH ASSOCIATION 1987
Japan Antibiotics Research Association
Subjects
Administration, Oral
Animals
Bacterial Infections - drug therapy
Biological and medical sciences
Cephalosporins - chemical synthesis
Cephalosporins - metabolism
Cephalosporins - therapeutic use
Chemical Phenomena
Chemistry
Esters
General pharmacology
Medical sciences
Mice
Pharmacology. Drug treatments
Physicochemical properties. Structure-activity relationships
Rats
Ester
Vertebrata
Mammalia
Structure activity relation
Mouse
Rodentia
Oral administration
Prodrug
Antibacterial agent
Biological activity
Cephalosporin
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Summary:The synthesis and the biological properties of orally active cephalosporin esters are described. 3-Methoxymethyl cephem derivatives having a 2-(2-aminothiazol-4-yl)-(Z)-2-methoxyiminoacetamide function at C-7 (1) showed good activity against a wide variety of bacteria including some β-lactamase producing species. The prodrug type esters of 1 exhibited a good urinary recovery after oral administration to mice and l-(isopropoxycarbonyloxy)ethyl ester (2a, CS-807) has been pre-clinically tested as an orally active cephem prodrug.
Bibliography:ObjectType-Article-1
SourceType-Scholarly Journals-1
ObjectType-Feature-2
content type line 23
ISSN:0021-8820
1881-1469
DOI:10.7164/antibiotics.40.370