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Related Experiment Videos

PD-140248 (Parke-Davis & Co).

M Steiert1, F J Schmitz

  • 1Institute for Medical Microbiology and Virology, University Hospital Düsseldorf, Germany.

Idrugs : the Investigational Drugs Journal
|August 19, 2005
PubMed
Summary
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PD-140248, a novel pyrrolidinyl naphthyridine, shows potent antibacterial activity against Gram-positive and quinolone-resistant bacteria. Its specific enantiomer exhibits enhanced efficacy, targeting further preclinical development for bacterial infections.

Area of Science:

  • Microbiology
  • Medicinal Chemistry
  • Pharmacology

Background:

  • PD-140248 is an investigational isomerase and topoisomerase II inhibitor developed for bacterial infections.
  • It belongs to the pyrrolidinyl naphthyridine class, designed to combat quinolone-resistant bacteria.

Purpose of the Study:

  • To evaluate the antibacterial spectrum and potency of PD-140248.
  • To compare the activity of different stereoisomers of PD-140248.

Main Methods:

  • In vitro susceptibility testing (MIC90) against various Gram-positive and Gram-negative bacteria.
  • In vitro and in vivo comparison of PD-140248 enantiomers against stereoisomers.

Main Results:

  • PD-140248 demonstrated broad-spectrum activity, particularly against Gram-positive bacteria like Staphylococcus and Streptococcus species.

Related Experiment Videos

  • It showed significant activity against quinolone-resistant strains, including methicillin- and ciprofloxacin-resistant S. aureus.
  • The (3R,1S) enantiomer of PD-140248 displayed 1- to 10-fold enhanced activity compared to its stereoisomers.

    • Conclusions:

    • PD-140248 exhibits potent in vitro antibacterial activity, especially against Gram-positive pathogens.
    • The specific enantiomer, (3R,1S)-PD-140248, warrants further preclinical investigation due to its superior efficacy.