Studies on cephalosporin antibiotics. VI. Synthesis, antibacterial activity and oral efficacy in mice of new 7 beta-[(Z)-2-(2-aminothiazol-4-yl)-2-(hydroxyimino)-acetamido]-3- (substituted alkylthio)cephalosporins
| Autor: | Hiroshi Fukushima, Akira Onodera, Kazuo Numata, Takatoshi Nagate, Chihiro Yokoo |
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| Rok vydání: | 1992 |
| Předmět: |
Pharmacology
Male Cephem Stereochemistry medicine.drug_class Chemistry Cephalosporin Administration Oral Blood Proteins Microbial Sensitivity Tests Prodrug Pivaloyloxymethyl Intestinal absorption Cephalosporins Rats Mice Structure-Activity Relationship Intestinal Absorption Drug Discovery medicine Animals Rats Wistar Antibacterial activity Cephalosporin Antibiotic Antibacterial agent |
| Zdroj: | The Journal of antibiotics. 45(9) |
| ISSN: | 0021-8820 |
| Popis: | A series of new 7 beta-[(Z)-2-(2-aminothiazol-4-yl)-2-(hydroxyimino)acetamido] cephalosporins (1) having various substituted alkylthio groups at the C-3 position of the cephem nucleus were prepared and evaluated for antibacterial activity and oral absorption in rats. Of these, the cephalosporin with a cyanomethylthio group (1a) showed the greatest activity against Staphylococcus aureus and Gram-negative bacteria. Its pivaloyloxymethyl ester (6a), a representative prodrug, exhibited good in vivo efficacy in mice by oral administration. The structure-activity relationships of 1 are also presented. |
| Databáze: | OpenAIRE |
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