Literature DB >> 22579486

Acylprolinamides: a new class of peptide deformylase inhibitors with in vivo antibacterial activity.

Jeffrey M Axten1, Jesús R Medina, Charles W Blackledge, Céline Duquenne, Seth W Grant, Mark A Bobko, Tony Peng, William H Miller, Theresa Pinckney, Timothy F Gallagher, Swarupa Kulkarni, Thomas Lewandowski, Glenn S Van Aller, Rimma Zonis, Paris Ward, Nino Campobasso.   

Abstract

A new class of PDF inhibitor with potent, broad spectrum antibacterial activity is described. Optimization of blood stability and potency provided compounds with improved pharmacokinetics that were suitable for in vivo experiments. Compound 5c, which has robust antibacterial activity, demonstrated efficacy in two respiratory tract infection models.
Copyright © 2012 Elsevier Ltd. All rights reserved.

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Year:  2012        PMID: 22579486     DOI: 10.1016/j.bmcl.2012.04.086

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


  1 in total

1.  A unique peptide deformylase platform to rationally design and challenge novel active compounds.

Authors:  Sonia Fieulaine; Rodolphe Alves de Sousa; Laure Maigre; Karim Hamiche; Mickael Alimi; Jean-Michel Bolla; Abbass Taleb; Alexis Denis; Jean-Marie Pagès; Isabelle Artaud; Thierry Meinnel; Carmela Giglione
Journal:  Sci Rep       Date:  2016-10-20       Impact factor: 4.379

  1 in total

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