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Bioorg Med Chem Lett. 2003 Feb 24;13(4):665-8.

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

Author information

1
GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, UK. richard_l_jarvest@gsk.com

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.

PMID:
12639554
DOI:
10.1016/s0960-894x(02)01027-2
[Indexed for MEDLINE]

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