Studies on .BETA.-lactam antibiotics. III. Syntheses and antibacterial activities of new 3-(1,3-dithiolan-2-yl)cephalosporins, ym-22508, ym-16457 and their prodrug-type esters
| Autor: | Noriaki Nagano, Masato Satoh, Ryuichiro Hara |
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| Rok vydání: | 1991 |
| Předmět: |
Chemical Phenomena
Streptococcus pyogenes medicine.drug_class Stereochemistry Antibiotics Cephalosporin medicine.disease_cause Mice chemistry.chemical_compound In vivo Streptococcal Infections Drug Discovery medicine Animals Escherichia coli Escherichia coli Infections Pharmacology Molecular Structure Staphylococcal Infections Prodrug Anti-Bacterial Agents Cephalosporins Chemistry Kinetics chemistry Staphylococcus aureus Lactam |
| Zdroj: | The Journal of Antibiotics. 44:422-428 |
| ISSN: | 1881-1469 0021-8820 |
| Popis: | The syntheses and biological activities of new 7-beta-[(Z)-2-(2-amino-4-thiazolyl)-2-hydroxy-iminoacetamido]-3-(1 ,3- dithiolan-2-yl)-3-cephem-4-carboxylic acid (YM-22508, 1a), 7-beta-[(Z)-2-(2-amino-4-thiazolyl)-2- methoxyiminoacetamido]-3-(1,3-dithiolan-2-yl)-3-cephem-4-carboxyli c acid (YM-16457, 1d) and their prodrug-type esters are described. Among them, YM-22561 (1c), the 1-acetoxyethyl ester of 1a, showed good in vivo efficacy in mice against infections of Staphylococcus aureus Smith, Streptococcus pyogenes S 23 and Escherichia coli NY-17 and a long plasma T1/2 in mice. |
| Databáze: | OpenAIRE |
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