Targeting methionyl tRNA synthetase: design, synthesis and antibacterial activity against Clostridium difficileof novel 3-biaryl-N-benzylpropan-1-amine derivatives

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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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
Date Type:	Publication
Status:	Published
Schools:	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:	23 Nov 2024 19:45
URI:	https://orca.cardiff.ac.uk/id/eprint/87911

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