Author/Authors :
Richard L. Jarvest، نويسنده , , Sula A Armstrong، نويسنده , , John M Berge، نويسنده , , Pamela Brown، نويسنده , , John S Elder، نويسنده , , Murray J Brown، نويسنده , , Royston C.B Copley، نويسنده , , Andrew K. Forrest، نويسنده , , Dieter W. Hamprecht، نويسنده , , Peter J OʹHanlon، نويسنده , , Darren J. Mitchell، نويسنده , , Stephen Rittenhouse، نويسنده , , David R. Witty، نويسنده ,
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.
