Inhibitors of bacterial tyrosyl tRNA synthetase: synthesis of carbocyclic analogues of the natural product SB-219383

R L Jarvest; J M Berge; C S Houge-Frydrych; L M Mensah; P J O'Hanlon; A J Pope

doi:10.1016/s0960-894x(01)00475-9

Inhibitors of bacterial tyrosyl tRNA synthetase: synthesis of carbocyclic analogues of the natural product SB-219383

Bioorg Med Chem Lett. 2001 Sep 17;11(18):2499-502. doi: 10.1016/s0960-894x(01)00475-9.

Authors

R L Jarvest¹, J M Berge, C S Houge-Frydrych, L M Mensah, P J O'Hanlon, A J Pope

Affiliation

¹ GlaxoSmithKline Pharmaceuticals, New Frontiers Science Park, Third Avenue, Harlow, CM19 5AW, Essex, UK.

PMID: 11549455
DOI: 10.1016/s0960-894x(01)00475-9

Abstract

Carbocyclic analogues of the microbial metabolite SB-219383 have been synthesised and evaluated as inhibitors of bacterial tyrosyl tRNA synthetase. One compound showed highly potent and selective nanomolar inhibition.

MeSH terms

Anti-Bacterial Agents / chemistry
Anti-Bacterial Agents / pharmacology
Biochemistry / methods
Bridged Bicyclo Compounds, Heterocyclic / chemistry*
Drug Design
Drug Evaluation, Preclinical
Enzyme Inhibitors / chemistry*
Enzyme Inhibitors / pharmacology*
Furans / chemistry*
Staphylococcus aureus / enzymology
Tyrosine / analogs & derivatives*
Tyrosine / chemistry*
Tyrosine-tRNA Ligase / antagonists & inhibitors*

Substances

Anti-Bacterial Agents
Bridged Bicyclo Compounds, Heterocyclic
Enzyme Inhibitors
Furans
SB 219383
Tyrosine
Tyrosine-tRNA Ligase