Literature DB >> 14623006

Alpha-substituted hydroxamic acids as novel bacterial deformylase inhibitor-based antibacterial agents.

R Jain1, A Sundram, S Lopez, G Neckermann, C Wu, C Hackbarth, D Chen, W Wang, N S Ryder, B Weidmann, D Patel, J Trias, R White, Z Yuan.   

Abstract

We report the synthesis and biological activity of analogues of VRC3375 (N-hydroxy-3-R-butyl-3-[(2-S-(tert-butoxycarbonyl)-pyrrolidin-1-ylcarbonyl]propionamide), an orally active peptide deformylase inhibitor. This study explores the structure-activity relationship of various chelator groups, alpha substituents, P(2)' and P(3)' substituents in order to achieve optimal antibacterial activity with minimal toxicity liability.

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Year:  2003        PMID: 14623006     DOI: 10.1016/j.bmcl.2003.07.020

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  3 in total

1.  Design and synthesis of macrocyclic peptidyl hydroxamates as peptide deformylase inhibitors.

Authors:  Gang Shen; Jinge Zhu; Anthony M Simpson; Dehua Pei
Journal:  Bioorg Med Chem Lett       Date:  2007-12-10       Impact factor: 2.823

2.  Peptide deformylase inhibitors as antibacterial agents: identification of VRC3375, a proline-3-alkylsuccinyl hydroxamate derivative, by using an integrated combinatorial and medicinal chemistry approach.

Authors:  D Chen; C Hackbarth; Z J Ni; C Wu; W Wang; R Jain; Y He; K Bracken; B Weidmann; D V Patel; J Trias; R J White; Z Yuan
Journal:  Antimicrob Agents Chemother       Date:  2004-01       Impact factor: 5.191

3.  Drug forecast - the peptide deformylase inhibitors as antibacterial agents.

Authors:  David R P Guay
Journal:  Ther Clin Risk Manag       Date:  2007-08       Impact factor: 2.423

  3 in total

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