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Comparative Study
. 2003 Aug 18;13(16):2709-13.
doi: 10.1016/s0960-894x(03)00532-8.

Structure-activity relationships of the peptide deformylase inhibitor BB-3497: modification of the methylene spacer and the P1' side chain

Stephen J Davies  1 , Andrew P Ayscough, R Paul Beckett, Ryan A Bragg, John M Clements, Sheila Doel, Christine Grew, Steven B Launchbury, Gemma M Perkins, Lisa M Pratt, Helen K Smith, Zoë M Spavold, S Wayne Thomas, Richard S Todd, Mark Whittaker
Affiliations
Comparative Study

Structure-activity relationships of the peptide deformylase inhibitor BB-3497: modification of the methylene spacer and the P1' side chain

Stephen J Davies et al. Bioorg Med Chem Lett. .

Abstract

Structural modifications to the peptide deformylase inhibitor BB-3497 are described. In this paper, we describe the initial SAR around this lead for modifications to the methylene spacer and the P1' side chain. Enzyme inhibition and antibacterial activity data revealed that the optimum distance between the N-formyl hydroxylamine metal binding group and the P1' side chain is one unsubstituted methylene unit. Additionally, lipophilic P1' side chains that closely mimic the methionine residue in the substrate provided compounds with the best microbiological profile.

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