Abstract
A series of alpha-methylene penicillins was synthesized and SAR were studied. The alpha-isomers were found to be chemically reactive and biologically active in contrast to the beta-isomers. In addition, the alpha-isomers have broader spectrum of in vitro activity than the corresponding penicillins. Generally, the alpha-isomers are more active against gram-negative bacteria than the corresponding penicillins, but slightly weaker in potency towards gram-positive organisms.
MeSH terms
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Anti-Bacterial Agents / chemical synthesis
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Anti-Bacterial Agents / chemistry
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Anti-Bacterial Agents / pharmacology
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Bacterial Proteins*
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Carrier Proteins / metabolism
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Gram-Negative Bacteria / drug effects
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Gram-Positive Bacteria / drug effects
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Hexosyltransferases*
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In Vitro Techniques
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Magnetic Resonance Spectroscopy
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Microbial Sensitivity Tests
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Molecular Structure
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Muramoylpentapeptide Carboxypeptidase / metabolism
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Penicillin G / analogs & derivatives*
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Penicillin G / chemical synthesis
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Penicillin G / chemistry
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Penicillin G / pharmacology
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Penicillin-Binding Proteins
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Penicillins / chemical synthesis*
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Penicillins / chemistry
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Penicillins / pharmacology
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Peptidyl Transferases*
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Structure-Activity Relationship
Substances
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Anti-Bacterial Agents
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Bacterial Proteins
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Carrier Proteins
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Penicillin-Binding Proteins
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Penicillins
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2,3-methylene penam
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Peptidyl Transferases
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Hexosyltransferases
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Muramoylpentapeptide Carboxypeptidase
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Penicillin G