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G. V. Lebedev, V. G. Grigorenko, R. L Antipin., M. Yu. Rubtsova, A. M. Egorov

Novel chromogenic substrate for bacterial beta-lactamases based on cephalosporin functionalized with epoxy group

Abstract

Beta-lactamases are the key enzymes involved in resistance towards beta-lactam antibiotics in pathogenic bacteria. Beta-lactamase inhibitor discovery process and study of resistance mechanisms force the search for new chromogenic substrates of beta-lactamases. For these purposes, a novel cephalosporin derivative with an epoxy functional group, called CMPD1, has been proposed and synthesized. This compound was shown to be hydrolyzed by TEM type beta-lactamases with a formation of a colored product with a maximum absorption at 450 nm. The difference in the maximum absorption of substrate and the product is 95 nm, which exceeds the value for the substrates previously described. It was found that the CMPD1 compound is hydrolyzed only by TEM type beta-lactamases which do not have mutations in the active site, which can be used to study the mechanisms of catalytic action of beta-lactamases.
Key words: beta-lactamases, chromogenic substrate, cephalosporin, epoxy group, antibiotic resistance.
Moscow University Chemistry Bulletin.
2018, Vol. 59, No. 2, P. 111
   

Copyright (C) Chemistry Dept., Moscow State University, 2002
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