Studies on 6 alpha-substituted penicillins. II. Synthesis and structure-activity relationships of 6 beta-(2-aryl-2-sulfoacetamido)-6 alpha-methoxy penicillanic acids
| Autor: | Kenyon Robert Fletcher, Desmond John Best, Andrew G. Lashford, Ronald A. Dixon, George Burton |
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| Rok vydání: | 1986 |
| Předmět: |
Pharmacology
biology Bicyclic molecule Chemical Phenomena Stereochemistry Aryl Penicillin Resistance Biological activity Penicillin G Microbial Sensitivity Tests biology.organism_classification chemistry.chemical_compound Chemistry Structure-Activity Relationship chemistry Enterobacteriaceae Drug Discovery Pseudomonas aeruginosa Sulbenicillin Lactam Penicillanic Acid Antibacterial activity Antibacterial agent Pseudomonadaceae |
| Zdroj: | The Journal of antibiotics. 39(10) |
| ISSN: | 0021-8820 |
| Popis: | The synthesis and antibacterial activity of 6 alpha-methoxysulbenicillin analogues (2) are described. Structure-activity studies of these derivatives bearing hydrophilic substituents in the phenyl ring led to the identification of disodium 6 beta-[D-2-(3,4-dihydroxyphenyl)-2-sulfoacetamido]-6 alpha-methoxypenicillanate (2m) as a compound with potent activity against Pseudomonas aeruginosa including beta-lactamase producing strains. Additional substitution of 2m gave derivatives 2p, 2q, 2r, with a further improvement in activity against Gram-negative bacteria. |
| Databáze: | OpenAIRE |
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