Targeting methionyl tRNA synthetase: design, synthesis and antibacterial activity against Clostridium difficile of novel 3-biaryl-Nbenzylpropan- 1-amine derivatives
Taylor and Francis
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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.
Journal of Enzyme Inhibition and Medicinal Chemistry;
Eissa, A.G., Blaxland, J.A., Williams, R.O., Metwally, K.A., El-Adl, S.M., Lashine, E.S.M., Baillie, L.W. and Simons, C. (2016) 'Targeting methionyl tRNA synthetase: design, synthesis and antibacterial activity against Clostridium difficile of novel 3-biaryl-N-benzylpropan-1-amine derivatives. Journal of enzyme inhibition and medicinal chemistry', 31(6), pp.1694-1697. DOI: 10.3109/14756366.2016.1140754.
Article published in Journal of Enzyme Inhibition and Medicinal Chemistry on 22 February 2016, available open access at: https://doi.org/10.3109/14756366.2016.1140754.