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Title: | Synthesis, structure, and analgesic properties of halogen-substituted 4-hydroxy-2,2-dioxo-1H-2λ 6 , 1-benzothiazine-3-carboxanilides |
Authors: | Ukrainets, I. V. Petrushova, L. A. Shishkina, S. V. Sidorenko, L. V. Sim, G. Kryvanych, O. V. Українець, І. В. Петрушова, Л. О. Шишкіна, С. В. Сидоренко, Л. В. Сім, Г. Криванич, О. В. |
Keywords: | amidation;2,1-benzothiazines;analgesia;anilide;synthesis;pain syndrome;4-hydroxy-2,2-dioxo-1H-2λ 6;1-benzothiazine-3-carboxamides;амідування;знеболювання;синтез;больовий синдром;4-гідрокси-2,2-діоксо-1Н-2λ 6;1-бензотіазін-3-карбоксамід;2,1-бензотіозини;анілід |
Issue Date: | 2016 |
Publisher: | Scientia Pharmaceutica |
Bibliographic description (Ukraine): | Synthesis, structure, and analgesic properties of halogen-substituted 4-hydroxy-2,2-dioxo-1H-2λ 6 , 1-benzothiazine-3-carboxanilides / I. V. Ukrainets, L. A. Petrushova, S. V. Shishkina et al. // Scientia Pharmaceutica. - 2016. - № 84. - p. 523–535. |
Abstract: | As potential new analgesics, the corresponding 4-hydroxy-2,2-dioxo-1H-2λ 6 ,1-benzothiazine- 3-carboxanilides have been obtained by amidation of ethyl 4-hydroxy-2,2-dioxo-1H-2λ 6 , 1-benzothiazine-3-carboxylate with aniline and its halogenated analogsin boiling dry xylene. The peculiarities of the mass and nuclear magnetic resonance (1H and 13C) spectra of the synthesized compounds are discussed. Using X-ray diffraction analysis, the ability of the compounds to form stable solvates with N,N-dimethylformamide has been shown on the example of 4-bromo-substituted derivative. It should be further studied to be considered in their crystallization. According to the results of the pharmacological testing conducted on the model of the thermal tail-flick (tail immersion test) among halogen-substituted 4-hydroxy-2,2-dioxo-1H-2λ 6 ,1-benzothiazine-3-carboxanilides, substances which are considerably superior to meloxicam and piroxicam by their analgesic activity have been found. They are of interest for further profound studies. |
URI: | http://dspace.nuph.edu.ua/handle/123456789/12389 |
Appears in Collections: | Наукові публікації кафедри фармацевтичної хімії |
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File | Description | Size | Format | |
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scipharm-84-00523.pdf | 3,15 MB | Adobe PDF | View/Open |
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