ASPARENOMYCINS A, B AND C, NEW CARBAPENEM ANTIBIOTICS V. INHIBITION OF β-LACTAMASES

Asparenomycins (ASMs) A, B and C inhibited a wide range of β-lactamases including both cephalosporinases and penicillinases usually at concentrations less than 3 μM. On studying the mechanism of inhibition of β-lactamases produced by Gram-negative bacteria by ASM A it was concluded that ASM A inhibi...

Full description

Saved in:
Bibliographic Details
Published in:Journal of antibiotics 1982, Vol.35(1), pp.39-45
Main Authors: MURAKAMI, KAZUHISA, DOI, MASAYOSHI, YOSHIDA, TADASHI
Format: Article
Language:English
Subjects:
Anti-Bacterial Agents - pharmacology
Bacteria - enzymology
beta-Lactamase Inhibitors
Drug Stability
Isoelectric Focusing
Kinetics
Substrate Specificity
Citations: Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:Asparenomycins (ASMs) A, B and C inhibited a wide range of β-lactamases including both cephalosporinases and penicillinases usually at concentrations less than 3 μM. On studying the mechanism of inhibition of β-lactamases produced by Gram-negative bacteria by ASM A it was concluded that ASM A inhibited the β-lactamases by acylating the enzymes. This conclusion was reached from the following observations. i) The inhibition was progressive with time. ii) The inhibitor formed stable complexes with the enzyme. iii) Before completing inhibition of one molecule of the enzyme, 1.8 molecules of the inhibitor were hydrolyzed.
ISSN:0021-8820
1881-1469
DOI:10.7164/antibiotics.35.39