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

Ahmed G. Eissa, James A. Blaxland, Rhodri O. Williams, Kamel A. Metwally, Sobhy M. El-Adl, El-Sayed M. Lashine, Leslie W. J. Baillie, Claire Simons
2016 Journal of Enzyme Inhibition and Medicinal Chemistry  
Claire 2016. Targeting methionyl tRNA synthetase: design, synthesis and antibacterial activity against Clostridium difficileof novel 3biaryl-N-benzylpropan-1-amine derivatives. Abstract The synthesis of a series of benzimidazole-N-benzylpropan-1-amines and adenine-Nbenzylpropan-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 g/mL. Molecular docking studies of
more » ... docking studies of the described amines determined that the amines interact within two active site pockets of Clostridium difficile methionyl tRNA synthetase with methoxy substituents in the benzyl ring and an adenine biaryl moiety resulting in optimal binding interactions.
doi:10.3109/14756366.2016.1140754 pmid:26899668 fatcat:dlz2a3y5nrco5jjbfo6e4nhzti