4-HYDROXY-2-QUINOLONES. 178. IRREVERSIBLE CHEMICAL MODIFICATION OF CHINOXICAINE AT THE POSITION 4 OF THE QUINOLONE RING

Authors

  • И. В. Украинец National University of Pharmacy
  • А. А. Ткач National University of Pharmacy
  • В. В. Кравцова National University of Pharmacy
  • В. И. Мамчур Dnepropetrovsk State Medical Academy
  • Е. Ю. Коваленко Dnepropetrovsk State Medical Academy

DOI:

https://doi.org/10.1007/3080

Keywords:

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

Abstract

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.

How to Cite
Ukrainets, I. V.; Tkach, A. A.; Kravtsova, V. V.; Mamchur, V. I.; Kovalenko, E. Yu. Chem. Heterocycl. Compd. 2010, 46, 850. [Khim. Geterotsikl. Soedin. 2010, 1050.]

For this article in the English edition see DOI 10.1007/s10593-010-0593-z

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Published

2016-02-24

Issue

No. 7 (2010)

Section

Original Papers