SEMISYNTHETIC PENICILLINS. A STRUCTURE -ACTIVITY STUDY OF A NEW SERIES OF ACYL AMINO ACID- PYRIDONE AND PYRIMIDONE AMOXICILLIN ANALOGS

The synthesis and biological activities of a series of 12 new semisynthetic penicillins is described. These compounds consisted of acylated amino acid analogs of 6-substituted-1, 2-dihydro-2-oxonicotinic acid and 2-substituted-3, 4-dihydro-4-oxo-5-pyrimidinecarboxylic acid attached to amoxicillin. T...

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Published inJournal of antibiotics Vol. 34; no. 7; pp. 862 - 868
Main Authors HASKEL, T. H., WOO, P. W. K., NICOLAIDES, E. D., HUTT, M. P., HUANG, G. G., SANCHEZ, J. P., DEJOHN, D., HEIFETZ, C. L., KROLLS, U., LUNNEY, E., MICH, T. F.
Format Journal Article
LanguageEnglish
Published Japan JAPAN ANTIBIOTICS RESEARCH ASSOCIATION 1981
Subjects
Amoxicillin - analogs & derivatives
Amoxicillin - pharmacology
Bacteria - drug effects
Microbial Sensitivity Tests
Structure-Activity Relationship
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Summary:The synthesis and biological activities of a series of 12 new semisynthetic penicillins is described. These compounds consisted of acylated amino acid analogs of 6-substituted-1, 2-dihydro-2-oxonicotinic acid and 2-substituted-3, 4-dihydro-4-oxo-5-pyrimidinecarboxylic acid attached to amoxicillin. The effect of the amino acid substituent, chirality of amino acid and acyl function on biological properties is discussed.
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ISSN:0021-8820
1881-1469
DOI:10.7164/antibiotics.34.862