Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 26, Issue 6, Pages 1589-1593Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2016.02.007
Keywords
Metallo-beta-lactamase; IMP-1 inhibitor; Captopril; Antibiotic resistance
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Funding
- Universiti Malaysia Sarawak, Malaysia
- National Health and Medical Research Council (NHMRC) of Australia [APP1084778]
- Australian Research Council [FT120100694]
- Australian Research Council [FT120100694] Funding Source: Australian Research Council
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A number of captopril analogues were synthesised and tested as inhibitors of the metallo-beta-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. (C) 2016 Elsevier Ltd. All rights reserved.
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