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Bioorg Med Chem Lett. 2003 Apr 7;13(7):1265-8.

Conformational restriction of methionyl tRNA synthetase inhibitors leading to analogues with potent inhibition and excellent gram-positive antibacterial activity.

Author information

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

Abstract

Conformationally restricted analogues of the central linker unit of bacterial methionyl tRNA synthetase (MRS) inhibitors have been prepared. The (1S,2R)-cyclopentylmethyl moiety was identified as the preferred cyclic linker, with significant diastereo- and enantioselectivity of activity. Combination of this linker with an optimal substituted aryl right-hand side has resulted in a compound with exceptionally good antibacterial activity against staphylococci and enterococci, including antibiotic resistant strains.

PMID:
12657260
DOI:
10.1016/s0960-894x(03)00093-3
[Indexed for MEDLINE]

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