Identification of novel potent bicyclic peptide deformylase inhibitors.
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Molteni, Valentina, He, Xiaohui, Nabakka, Juliet, Yang, Kunyong, Kreusch, Andreas, Gordon, P., Bursulaya, Badry, Warner, Ian, Shin, Tanya, Biorac, Tanya, Ryder, Neil, Goldberg, Ronald, 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 |