Structure--activity relationships in cephalosporins prepared from penicillins. 1. 7beta-Acylamino derivatives of 3-benzyl- and 3-(3-pyridylmethyl)ceph-3-em-4-carboxylic acids
Autor: | R. Sutherland, M. J. Basker, Robert Southgate, Michael J. Pearson, Terence C. Smale, Patricia Tolliday, John H. C. Nayler, Edward G. Brain, Neal F. Osborne, A. J. Eglington |
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Rok vydání: | 1977 |
Předmět: |
Staphylococcus aureus
medicine.drug_class Chemistry Cephalosporin Microbial Sensitivity Tests Medicinal chemistry Cephalosporins Penicillin Acylation Structure-Activity Relationship Drug Discovery Benzyl Compounds polycyclic compounds medicine Side chain Molecular Medicine Amine gas treating Antibacterial activity medicine.drug |
Zdroj: | Journal of medicinal chemistry. 20(8) |
ISSN: | 0022-2623 |
Popis: | tert-Butyl 7beta-aminoceph-3-em-4-carboxylates carrying either benzyl or 3-pyridylmethyl substituents at position 3 have been prepared by a multistep modification of the penicillin nucleus. Acylation of either amine, followed by deprotection, gave a range of new cephalosporins. The relationship between structure and antibacterial activity is discussed. D-Phenylglycine proved to be a preferred side chain in both series. |
Databáze: | OpenAIRE |
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