Literature DB >> 19487444

AFN-1252, a FabI inhibitor, demonstrates a Staphylococcus-specific spectrum of activity.

James A Karlowsky1, Nachum Kaplan, Barry Hafkin, Daryl J Hoban, George G Zhanel.   

Abstract

AFN-1252, a potent inhibitor of enoyl-acyl carrier protein reductase (FabI), inhibited all clinical isolates of Staphylococcus aureus (n = 502) and Staphylococcus epidermidis (n = 51) tested, including methicillin (meticillin)-resistant isolates, at concentrations of <or=0.12 microg/ml. In contrast, AFN-1252 was inactive (MIC(90), >4 microg/ml) against clinical isolates of Streptococcus pneumoniae, beta-hemolytic streptococci, Enterococcus spp., Enterobacteriaceae, nonfermentative gram-negative bacilli, and Moraxella catarrhalis. These data support the continued development of AFN-1252 for the treatment of patients with resistant staphylococcal infections.

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Year:  2009        PMID: 19487444      PMCID: PMC2715641          DOI: 10.1128/AAC.00400-09

Source DB:  PubMed          Journal:  Antimicrob Agents Chemother        ISSN: 0066-4804            Impact factor:   5.191


  6 in total

1.  A triclosan-resistant bacterial enzyme.

Authors:  R J Heath; C O Rock
Journal:  Nature       Date:  2000-07-13       Impact factor: 49.962

2.  Bacterial fatty acid biosynthesis: targets for antibacterial drug discovery.

Authors:  J W Campbell; J E Cronan
Journal:  Annu Rev Microbiol       Date:  2001       Impact factor: 15.500

3.  In vitro activity of API-1252, a novel FabI inhibitor, against clinical isolates of Staphylococcus aureus and Staphylococcus epidermidis.

Authors:  James A Karlowsky; Nancy M Laing; Trish Baudry; Nachum Kaplan; David Vaughan; Daryl J Hoban; George G Zhanel
Journal:  Antimicrob Agents Chemother       Date:  2007-01-12       Impact factor: 5.191

4.  Biochemical and genetic characterization of the action of triclosan on Staphylococcus aureus.

Authors:  C Slater-Radosti; G Van Aller; R Greenwood; R Nicholas; P M Keller; W E DeWolf; F Fan; D J Payne; D D Jaworski
Journal:  J Antimicrob Chemother       Date:  2001-07       Impact factor: 5.790

Review 5.  Inhibitors of fatty acid synthesis as antimicrobial chemotherapeutics.

Authors:  R J Heath; S W White; C O Rock
Journal:  Appl Microbiol Biotechnol       Date:  2002-03-07       Impact factor: 4.813

6.  Discovery of a novel and potent class of FabI-directed antibacterial agents.

Authors:  David J Payne; William H Miller; Valerie Berry; John Brosky; Walter J Burgess; Emile Chen; Walter E DeWolf; Andrew P Fosberry; Rebecca Greenwood; Martha S Head; Dirk A Heerding; Cheryl A Janson; Deborah D Jaworski; Paul M Keller; Peter J Manley; Terrance D Moore; Kenneth A Newlander; Stewart Pearson; Brian J Polizzi; Xiayang Qiu; Stephen F Rittenhouse; Courtney Slater-Radosti; Kevin L Salyers; Mark A Seefeld; Martin G Smyth; Dennis T Takata; Irene N Uzinskas; Kalindi Vaidya; Nicola G Wallis; Scott B Winram; Catherine C K Yuan; William F Huffman
Journal:  Antimicrob Agents Chemother       Date:  2002-10       Impact factor: 5.191

  6 in total
  34 in total

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10.  AFN-1252 is a potent inhibitor of enoyl-ACP reductase from Burkholderia pseudomallei--Crystal structure, mode of action, and biological activity.

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Journal:  Protein Sci       Date:  2015-04-02       Impact factor: 6.725

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