2,1-BENZOTHIAZINE-2,2-DIOXIDES. 4. SYNTHESIS, STRUCTURE, AND ANALGESIC PROPERTIES OF 4-HYDROXY-1-METHYL-<i>N</i>-(PYRIDIN-2-YL)-2,2-DIOXO-1<i>H</i>-2<sup>6</sup>,1-BENZOTHIAZINE-3-CARBOXAMIDES

Authors

  • И. В. Украинец Национальный фармацевтический университет
  • Л. А. Петрушова Национальный фармацевтический университет
  • С. П. Дзюбенко Винницкий национальный медицинский университет им. Н. И. Пирогова
  • Л. Янян Чанчуньский медицинский колледж

DOI:

https://doi.org/10.1007/1331

Keywords:

amides, 2-aminopyridine, 2-aminopyrazine, 2-aminopyrimidine, 2, 1-benzothiazines, analgesic activity

Abstract

An improved method for the reaction of methyl-4-hydroxy-1-methyl-2,2-dioxo-1Н-2λ6,1-benzothiazine-3-carboxylate with hetaryl amines, which allows to obtain 4-hydroxy-1-methyl-2,2‑dioxo-N-(pyridin-2-yl)-1Н-2λ6,1-benzothiazine-3-carboxamides in good yields and with high purity. It was shown by x-ray analysis that the synthesized compounds exist in the zwitter-ion form. The mass spectra indicate their propensity to SO2 extrusion. In the pharmacological tests, rpomising compounds were found with analgesic activities exceeding those of known oxicam type drugs.

How to Cite
Ukrainets, I. V.; Petrushova, L. A.; Dzyubenko, S. P.; Liu Yangyang Chem. Heterocycl. Compd. 2014, 50, 564. [Khim. Geterotsikl. Soedin. 2014, 614.]

For this article in the English edition see DOI 10.1007/s10593-014-1508-1

Published

2014-04-23

Issue

Section

Original Papers