Studies on monocyclic .BETA.-lactam antibiotics. II. Synthesis and antibacterial activity of 3-acylamino-2-azetidinone-1-oxysulfonic acids
| Autor: | Tetsumi Kitani, Katsuyuki Nagumo, Takako Hori, Yoshikazu Fukuoka, Chosaku Yoshida, Saikawa Isamu, Kaishu Momonoi, Joji Nakano |
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| Rok vydání: | 1985 |
| Předmět: |
Pharmacology
Bacteria biology Chemistry Stereochemistry Substituent Biological activity Microbial Sensitivity Tests beta-Lactams biology.organism_classification Anti-Bacterial Agents Structure-Activity Relationship chemistry.chemical_compound Drug Discovery Lactam Structure–activity relationship Antibacterial activity Enterobacter cloacae Antibacterial agent |
| Zdroj: | The Journal of Antibiotics. 38:1536-1549 |
| ISSN: | 1881-1469 0021-8820 |
| DOI: | 10.7164/antibiotics.38.1536 |
| Popis: | The synthesis and in vitro antibacterial and beta-lactamase inhibitory activity of the 2-azetidinone-1-oxysulfonic acids having a substituent at C-4 position of the beta-lactam ring are described. The influence of C-4 substituents on the antibacterial activity was examined for the compounds having alpha-ureidoacetyl or alpha-oxyiminoacetyl group as acyl side chain at C-3 position. The antibacterial activity is correlated with the C-4 substituents and acyl side chain. Especially, 4(R)-methyl substituted derivatives exhibited excellent activity against Gram-negative bacteria and 4-dimethyl substituted derivatives exhibited strong activity against resistant Gram-negative bacteria except for Pseudomonas aeruginosa. 39 and 40 showed strong inhibitory activity against cephalosporinase of Enterobacter cloacae H-27. |
| Databáze: | OpenAIRE |
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