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ID: ALA1136587

Journal: Bioorg Med Chem Lett

Title: Optimisation of aryl substitution leading to potent methionyl tRNA synthetase inhibitors with excellent gram-positive antibacterial activity.

Authors: Jarvest RL, Berge JM, Brown MJ, Brown P, Elder JS, Forrest AK, Houge-Frydrych CS, O'Hanlon PJ, McNair DJ, Rittenhouse S, Sheppard RJ.

Abstract: Optimisation of the left-hand-side aryl moiety of a file compound screening hit against Staphylococcus aureus methionyl tRNA synthetase led to the identification of a series of potent nanomolar inhibitors. The best compounds showed excellent antibacterial activity against staphylococcal and enterococcal pathogens, including strains resistant to clinical antibiotics.

CiteXplore: 12639554

DOI: 10.1016/s0960-894x(02)01027-2