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[摘要]：Penicillin-binding proteins (PBPs) are important bacterial enzymes that carry out the final steps of bacterial cell wall assembly. Their DD-transpeptidase activity accomplishes the essential peptide cross linking step of the cell wall. To date, all attempts to discover effective inhibitors of PBPs, apart from beta-lactams, have not led to new antibiotics. Therefore, the need for new classes of efficient inhibitors of these enzymes remains. Guided by a computational fragment based docking procedure, carried out on Escherichia cob PBPS, we have designed and synthesized a series of 4-quinolones as potential inhibitors of PBPs. We describe their binding to the PBPs of E cob and Bacillus subtilis. Notably, these compounds bind quite tightly to the essential high molecular mass PBPs. |
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