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 Figshare  
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
more » ... nine biaryl moiety resulting in optimal binding interactions.
doi:10.6084/m9.figshare.2574859 fatcat:whykpq6pyvhenbxqvnu2ilujcq