Preparation and structure-activity relationships of some 6 alpha-substituted penicillins
| Autor: | Desmond John Best, Michael J. Basker, Ronald A. Dixon, George Burton, Frank P. Harrington, Kenyon Robert Fletcher, Andrew W. Taylor, Peter H. Bentley, Andrew G. Lashford |
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| Rok vydání: | 1985 |
| Předmět: |
Pharmacology
biology Chemistry Stereochemistry Aryl Penicillins Carbenicillin biology.organism_classification Enterobacteriaceae chemistry.chemical_compound Structure-Activity Relationship Drug Discovery Sulbenicillin Pseudomonas aeruginosa medicine Lactam Antibacterial activity Antibacterial agent Piperacillin medicine.drug |
| Zdroj: | The Journal of antibiotics. 38(6) |
| ISSN: | 0021-8820 |
| Popis: | The influence on the antibacterial activity of introducing a 6 alpha-methoxy group into carbenicillin, and various 6 alpha-substituents into sulbenicillin and piperacillin was examined. Further variations of the side chain aryl group were examined in the 6 alpha-methoxy substituted series. This led to the identification of disodium 6 beta-(D,L-2-carboxy-2-thien-3-ylacetamido)-6 alpha-methoxypenicillanate (5b) as a beta-lactamase stable derivative with useful activity against Enterobacteriaceae, and disodium 6 beta-[D-2-(4-aminophenyl)-2-sulfoacetamido]-6 alpha-methoxypenicillanate (6e) with slightly lower activity against the Enterobacteriaceae but more active against Pseudomonas aeruginosa. |
| Databáze: | OpenAIRE |
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