AI Article Synopsis
- Researchers identified effective inhibitors of bacterial methionyl tRNA synthetase (MRS) using structure-activity relationship (SAR) studies focused on the quinolone structure.
- They found that a specific NH-C-NH feature in a bicyclic heteroaromatic system is crucial for MRS inhibition.
- One compound, referred to as Compound 46, showed strong antibacterial effects against antibiotic-resistant staphylococci and enterococci strains.
Article 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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| http://dx.doi.org/10.1016/j.bmcl.2004.05.070 | DOI Listing |
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