Structure-activity Relationships for Interactions between Carbapenems and β-Lactamases

Carbapenems are one of the novel class of beta -lactams recently developed. They have excellent antibacterial activity and a wide spectrum against both Gram-positive and Gram-negative bacteria. This high activity is due to good diffusion through the outer membrane in Gram-negative organisms, high af...

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Published inJournal of antibiotics Vol. 48; no. 2; pp. 188 - 190
Main Authors SUMITA, YOSHIHIRO, NOUDA, HIROSHI, SHINAGAWA, HISATOSHI, YAMAGA, HIROSHI, SUNAGAWA, MAKOTO
Format Journal Article
LanguageEnglish
Published Tokyo JAPAN ANTIBIOTICS RESEARCH ASSOCIATION 1995
Japan Antibiotics Research Association
Subjects
Anti-Bacterial Agents - chemistry
Anti-Bacterial Agents - pharmacology
Antibacterial agents
Antibiotics. Antiinfectious agents. Antiparasitic agents
beta-Lactamases - chemistry
Biological and medical sciences
Carbapenems - chemistry
Gram-Negative Bacteria - drug effects
Gram-Positive Bacteria - drug effects
Medical sciences
Pharmacology. Drug treatments
Structure-Activity Relationship
Structure activity relation
Enzyme
Methyl group
Lactam
Hydrolases
Molecular interaction
β-Lactamase
Antibacterial agent
In vitro
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Summary:Carbapenems are one of the novel class of beta -lactams recently developed. They have excellent antibacterial activity and a wide spectrum against both Gram-positive and Gram-negative bacteria. This high activity is due to good diffusion through the outer membrane in Gram-negative organisms, high affinities for penicillin-binding proteins (PBPs) and high stability and inhibitory activity against beta -lactamases. However, carbapenems were hydrolyzed by dehydropeptidase-I (DHP-I) from several animals. In previous paper, we revealed that 1 beta -methyl moiety on meropenem had the important role of prevention from hydrolysis by DHP-I, furthermore, that 1 beta -methyl group on carbapenems affected the activity against Pseudomonas aeruginosa. Since, we have interested that the role of 1 beta -methyl moiety on several biological activities of carbapenems. In the present study, therefore, we examined the interactions between carbapenems and various beta -lactamases concerning structure-activity relationships, especially 1 beta -methyl moiety.
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ISSN:0021-8820
1881-1469
DOI:10.7164/antibiotics.48.188