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4-Hydroxy-2-quinolones. 195*. Synthesis of novel, potential analgesics based on 4-(hetarylmethyl)amino-2-oxo-1,2-dihydro-quinoline-3-carboxylic acids

  • I. V. UkrainetsEmail author
  • E. V. Mospanova
  • L. V. Savchenkova
  • S. I. Yankovich
Article

From the viewpoint of the method of bioisosteric replacement we have carried out the synthesis of a series of 4-(hetarylmethyl)amino-2-oxo-1,2-dihydroquinoline-3-carboxylic acids. For several examples it has been shown experimentally that the aromatic ring in the benzyl fragment of 4-benzylamino-2-oxo-1,2-dihydroquinoline-3-carboxylic acid can be replaced by an isosteric heterocycle without lowering the analgesic properties.

Keywords

4-N-R-2-oxo-1,2-dihydroquinoline-3-carboxylic acids analgesic activity bioisosteric replacement 

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Copyright information

© Springer Science+Business Media, Inc. 2011

Authors and Affiliations

  • I. V. Ukrainets
    • 1
    Email author
  • E. V. Mospanova
    • 2
  • L. V. Savchenkova
    • 3
  • S. I. Yankovich
    • 3
  1. 1.National Pharmaceutical UniversityKharkivUkraine
  2. 2.Institute of Chemical TechnologyV. Dal East-Ukrainian National UniversityRubizhneUkraine
  3. 3.Luhansk State Medical UniversityLuhanskUkraine

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