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Updated: Mar 25, 2026

The Use of a β-lactamase-based Conductimetric Biosensor Assay to Detect Biomolecular Interactions
Published on: February 1, 2018
Captopril analogues as metallo-β-lactamase inhibitors
Yusralina Yusof1, Daniel T C Tan1, Omid Khalili Arjomandi1
1School of Chemistry and Molecular Biosciences, The University of Queensland, Queensland 4072, Australia.
Abstract:
A number of captopril analogues were synthesised and tested as inhibitors of the metallo-β-lactamase IMP-1. Structure-activity studies showed that the methyl group was unimportant for activity, and that the potencies of these inhibitors could be best improved by shortening the length of the mercaptoalkanoyl side-chain. Replacing the thiol group with a carboxylic acid led to complete loss of activity, and extending the length of the carboxylate group led to decreased potency. Good activity could be maintained by substituting the proline ring with pipecolic acid.
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