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Acylprolinamides: a new class of peptide deformylase inhibitors with in vivo antibacterial activity |
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| Authors: | Axten Jeffrey M Medina Jesús R Blackledge Charles W Duquenne Céline Grant Seth W Bobko Mark A Peng Tony Miller William H Pinckney Theresa Gallagher Timothy F Kulkarni Swarupa Lewandowski Thomas Van Aller Glenn S Zonis Rimma Ward Paris Campobasso Nino |
| Affiliation: | Infectious Diseases Center of Excellence for Drug Discovery, Antibacterial Discovery Performance Unit, GlaxoSmithKline, Collegeville, PA 19426, USA. jeffrey.m.axten@gsk.com |
| 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. |
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