Eissa, Ahmed G., Blaxland, James A., Williams, Rhodri O., Metwally, Kamel A., El-Adl, Sobhy M., Lashine, El-Sayed M., Baillie, Les ORCID: https://orcid.org/0000-0002-8186-223X and Simons, Claire ORCID: https://orcid.org/0000-0002-9487-1100 2016. Targeting methionyl tRNA synthetase: design, synthesis and antibacterial activity against Clostridium difficileof novel 3-biaryl-N-benzylpropan-1-amine derivatives. Journal of Enzyme Inhibition and Medicinal Chemistry 31 (6) , pp. 1694-1697. 10.3109/14756366.2016.1140754 |
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Official URL: http://dx.doi.org/10.3109/14756366.2016.1140754
Abstract
The synthesis of a series of benzimidazole-N-benzylpropan-1-amines and adenine-N-benzylpropan-1-amines is described. Subsequent evaluation against two strains of the anaerobic bacterium Clostridium difficile was performed with three amine derivatives displaying MIC values of 16 μg/mL. Molecular docking studies of the described amines determined that the amines interact within two active site pockets of C. difficile methionyl tRNA synthetase with methoxy substituents in the benzyl ring and an adenine biaryl moiety resulting in optimal binding interactions
Item Type: | Article |
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Date Type: | Publication |
Status: | Published |
Schools: | Pharmacy |
Subjects: | R Medicine > RM Therapeutics. Pharmacology |
Uncontrolled Keywords: | 3-Biaryl-N-benzylpropan-1-amines, Clostridium difficile, MetRS–ligand interactions, methionyl-tRNA synthetase, molecular modelling |
Publisher: | Taylor & Francis |
ISSN: | 1475-6366 |
Date of First Compliant Deposit: | 30 March 2016 |
Date of Acceptance: | 5 January 2016 |
Last Modified: | 07 Nov 2023 18:11 |
URI: | https://orca.cardiff.ac.uk/id/eprint/87911 |
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