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Identification of novel potent bicyclic peptide deformylase inhibitors.

Molteni, Valentina and He, Xiaohui and Nabakka, Juliet and Yang, Kunyong and Kreusch, Andreas and Gordon, P. and Bursulaya, Badry and Warner, Ian and Shin, Tanya and Biorac, Tanya and Ryder, Neil and Goldberg, Ronald and Doughty, John and He, Yun (2004) Identification of novel potent bicyclic peptide deformylase inhibitors. Bioorganic & Medicinal Chemistry Letters, 14 (6). pp. 1477-1481. ISSN 0960-894X

Abstract

Screening of our compound collection using Staphylococcus aureus Ni-Peptide deformylase (PDF) afforded a very potent PDF inhibitor with an IC(50) 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 attempting to improve antibacterial activity. Many of the compounds synthesized proved to be excellent PDF-Ni inhibitors and some showed increased antibacterial activity in selected strains.

Item Type: Article
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Additional Information: author can archive post-print (ie final draft post-refereeing); Publisher's version/PDF cannot be used
Keywords: Peptide deformylase inhibitors
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Date Deposited: 14 Dec 2009 14:02
Last Modified: 31 Jan 2013 01:21
URI: https://oak.novartis.com/id/eprint/285

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