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Chemistry of Heterocyclic Compounds

, Volume 46, Issue 7, pp 850–855 | Cite as

4-hydroxy-2-quinolones. 178*. irreversible chemical modification of chinoxicaine at the position 4 of the quinolone ring

  • I. V. UkrainetsEmail author
  • A. A. Tkach
  • V. V. Kravtsova
  • V. I. Mamchur
  • E. Yu. Kovalenko
Article

While continuing our investigation in improving the pharmaceutical activities of the local anesthetic Chinoxicaine we have studied the irreversible replacement of its 4-OH group for bioisosteric fragments. For this purpose the synthesis of a series of 4-R-2-oxo-1,2-dihydroquinoline-3-carboxylic acids 2-(diethylamino)ethylamide hydrochlorides has been carried out. The experimental data of the local anesthetic properties of the compounds obtained are given and discussed.

Keywords

4-R-2-oxo-1,2-dihydroquinoline-3-carboxylic acids amidation bioisosteric replacement local anesthetics 

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Copyright information

© Springer Science+Business Media, Inc. 2010

Authors and Affiliations

  • I. V. Ukrainets
    • 1
    Email author
  • A. A. Tkach
    • 1
  • V. V. Kravtsova
    • 1
  • V. I. Mamchur
    • 2
  • E. Yu. Kovalenko
    • 2
  1. 1.National University of PharmacyKharkivUkraine
  2. 2.Dnepropetrovsk State Medical AcademyDnepropetrovskUkraine

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