Definition of the heterocyclic pharmacophore of bacterial methionyl tRNA synthetase inhibitors: potent antibacterially active non-quinolone analogues |
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| Authors: | Jarvest Richard L Armstrong Sula A Berge John M Brown Pamela Elder John S Brown Murray J Copley Royston C B Forrest Andrew K Hamprecht Dieter W O'Hanlon Peter J Mitchell Darren J Rittenhouse Stephen Witty David R |
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| Affiliation: | GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, Essex CM19 5AW, UK. richard.l.jarvest@gsk.com |
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| Abstract: | Potent inhibitors of bacterial methionyl tRNA synthetase (MRS) have previously been reported. Through SAR of the quinolone moiety, the right hand side pharmacophore for MRS inhibition has now been defined as an NH-C-NH functionality in the context of a bicyclic heteroaromatic system. Potent antibacterial fused-pyrimidone and fused-imidazole analogues have been obtained and enantioselective activity demonstrated. Compound 46 demonstrated very good antibacterial activity against panels of antibiotic-resistant staphylococci and enterococci. |
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