Identification of novel potent bicyclic peptide deformylase inhibitors

…, X He, J Nabakka, K Yang, A Kreusch, P Gordon…

文献索引：Molteni, Valentina; He, Xiaohui; Nabakka, Juliet; Yang, Kunyong; Kreusch, Andreas; Gordon, Perry; Bursulaya, Badry; Warner, Ian; Shin, Tanya; Biorac, Tanya; Ryder, Neil S.; Goldberg, Ron; Doughty, John; He, Yun Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 6 p. 1477 - 1481

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被引用次数: 40

摘要

Screening of our compound collection using Staphylococcus aureus Ni–Peptide deformylase (PDF) afforded a very potent PDF inhibitor with an IC50 in the low nanomolar range but with poor antibacterial activity (MIC). Three-dimensional structural information obtained from Pseudomonas aeruginosa Ni–PDF complexed with the inhibitor suggested the synthesis of a variety of analogues that would maintain high binding affinity while ...