Advanced search
Publication Cover
Journal of Chemotherapy Volume 25, 2013 - Issue 1
Submit an article Journal homepage
1,110
Views
28
CrossRef citations to date
0
Altmetric
Antimicrobial Original Research Paper

In vitro activity (MICs and rate of kill) of AFN-1252, a novel FabI inhibitor, in the presence of serum and in combination with other antibiotics

Nachum Kaplan Affinium PharmaceuticalsInc., Toronto, ON, Canada,Correspondence[email protected]
,
Donald Awrey Campbell Family Institute for Breast Cancer ResearchToronto, ON, Canada
,
Elias BardouniotisSwitzerland Trade and Investment Promotion, Toronto, ON, Canada
,
Judd BermanDalton Medicinal ChemistryToronto, ON, Canada
,
Jeremy Yethon Sanofi PasteurCambridge, MA, USA
,
Henry W Pauls Campbell Family Institute for Breast Cancer ResearchToronto, ON, Canada
&
Barry Hafkin Affinium PharmaceuticalsInc., Toronto, ON, Canada,
 show all
Pages 18-25 | Published online: 12 Nov 2013

References

  • Miller WH, Seefeld MA, Newlander KA, Uzinskas IN, Burgess WJ, Heerding DA, et al.. Discovery of aminopyridine-based inhibitors of bacterial enoyl-ACP reductase (FabI). J Med Chem. 2002;45:3246–56.
  • Heath RJ, White SW, Rock CO. Inhibitors of fatty acid synthesis as antimicrobial chemotherapeutics. Appl Microbiol Biotechnol. 2002;58:695–703.
  • Kodali S, Galgoci A, Young K, Painter R, Silver LL, Herath KB, et al.. Determination of selectivity and efficacy of fatty acid synthesis inhibitors. J Biol Chem. 2005;280:1669–77.
  • Zhang Y-M, White SW, Rock CO. Inhibiting bacterial fatty acid synthesis. J Biol Chem. 2006;281:17541–4.
  • Lu H, Tonge PJ. Inhibitors of FabI, an enzyme drug target in the bacterial fatty acid biosynthesis pathway. Acc Chem Res. 2008;41:11–20.
  • Asturias FJ, Chadick JZ, Cheung IK, Stark H, Witkowski A, Joshi AK, et al.. Structure and molecular organization of mammalian fatty acid synthase. Nat Struct Mol Biol. 2005;12:225–32.
  • Kaplan N, Albert M, Awrey D, Bardouniotis E, Berman J, Clarke T, et al.. AFN-1252 - Mode of action, in vitro activity and in vivo efficacy of a selective anti-staphylococcal FabI inhibitor. Antimicrob Agents Chemother. 2012;56:5865–74.
  • Karlowsky JA, Kaplan N, Hafkin B, Hoban DJ, Zhanel GG. AFN-1252, a FabI inhibitor, demonstrates a Staphylococcus-specific spectrum of activity. Antimicrob Agents Chemother. 2009;53:3544–8.
  • Karlowsky JA, Laing NM, Baudry T, Kaplan N, Vaughan D, Hoban DJ, et al.. In vitro activity of API-1252, a novel FabI inhibitor, against clinical isolates of Staphylococcus aureus and Staphylococcus epidermidis. Antimicrob Agents Chemother. 2007;51:1580–1.
  • Clinical and Laboratory Standards Institute. Methods for dilution antimicrobial susceptibility tests for bacteria that grow aerobically – 9th ed. Approved Standard M7-A9. CLSI, Wayne, PA, USA, 2012.
  • Eliopoulous GM, Moellering RC. Antimicrobial combinations. In: Lorian V, editor. Antibiotics in laboratory medicine. 4th ed. Baltimore, MD: The Williams & Wilkins Co.; 1996. p. 330–96.
  • Meletiadis J, Mouton JW, te Dorsthorst DTA, Verweij PE. Assessing combination of antifungal drugs against yeasts and filamentous fungi: comparison of different drug interaction models. Med Mycol. 2005;43:133–52.
  • Merrikin DJ, Briant J, Rolinson GN. Effect of protein binding on antibiotic activity in vivo. J Antimicrob Chemother. 1983;11:233–8.
  • Kaplan N, Hafkin B. Tolerability, safety and pharmacokinetics of multiple oral doses of AFN-1252 in healthy subjects. Abstract F1 -1349. 51st ICAAC, Interscience Conference on Antimicrobial Agents and Chemotherapy, 2011 Sep 17–20; Chicago, IL, USA.
  • Silverman JA, Mortin LI, Vanpraagh AD, Li T, Alder J. Inhibition of daptomycin by pulmonary surfactant: in vitro modeling and clinical impact. J Infect Dis. 2005;191:2149.

Related research

People also read lists articles that other readers of this article have read.

Recommended articles lists articles that we recommend and is powered by our AI driven recommendation engine.

Cited by lists all citing articles based on Crossref citations.
Articles with the Crossref icon will open in a new tab.