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Title: | Two pseudo-enantiomeric forms of N -benzyl-4-hydroxy-1 methyl-2,2-dioxo-1 H -2λ6,1-benzothiazine-3-carboxamide and their analgesic properties |
Authors: | Ukrainets, I. V. Shishkina, S. V. Baumer, V. N. Gorokhova, O. V. Petrushova, L. A. Sim, G. Украинец, И. В. Шишкина, С. В. Баумер, В. Н. Горохова, О. В. Петрушова, Л. А. Сим, Г. Українець, І. В. Шишкіна, С. В. Баумер, В. Н. Горохова, О. В. Петрушова, Л. О. Сім, Г. |
Keywords: | pharmaceutical compound;pharmacological study;crystal structure;2 6,1-benzothiazine3-carboxamide;antinociceptive activity;chiral crystals;analgesic activity;фармацевтична композиція;Фармакологічне дослідження;кристалічна структура; ; .;2,6,1-бензотіазин-3-карбоксамід;антиноцицептивна активність;хіральні кристали;анальгетична активність;фармацевтическое соединение;фармакологическое исследование;кристалическая структура;хиральные кристаллы;антиноцицептивная активность;анальгетическая активность |
Issue Date: | 2016 |
Publisher: | IUCr Journals |
Bibliographic description (Ukraine): | Ukrainets, I. V. Two pseudo-enantiomeric forms of N -benzyl-4-hydroxy-1 methyl-2,2-dioxo-1 H -2λ6,1-benzothiazine-3-carboxamide and their analgesic properties / I. V. Ukrainets, S. V. Shishkina, V. N. Baumer et. al. // Acta crystallographica. Section C. - 2016. - C72. - P. 411-417. |
Abstract: | The fact that molecular crystals exist as different polymorphic modifications and the identification of as many polymorphs as possible are important considerations for the pharmaceutic industry. The molecule of N-benzyl-4hydroxy-1-methyl-2,2-dioxo-1H-2 6,1-benzothiazine-3-carboxamide, C17H16N2O4S, does not contain a stereogenic atom, but intramolecular hydrogen-bonding interactions engender enantiomeric chiral conformations as a labile racemic mixture. The title compound crystallized in a solvent-dependent single chiral conformation within one of two conformationally polymorphic P212121 orthorhombic chiral crystals (denoted forms A and B). Each of these pseudoenantiomorphic crystals contains one of two pseudo-enantiomeric diastereomers. Form A was obtained from methylene chloride and form B can be crystallized from N,N-dimethylformamide, ethanol, ethyl acetate or xylene. Pharmacological studies with solid–particulate suspensions have shown that crystalline form A exhibits an almost fourfold higher antinociceptive activity compared to form B. |
Description: | DOI: 10.1107/S2053229616005453 |
URI: | http://dspace.nuph.edu.ua/handle/123456789/13428 |
Appears in Collections: | Наукові публікації кафедри фармацевтичної хімії |
Files in This Item:
File | Description | Size | Format | |
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2016.03_стаття_Українець І.В. Acta Cryst.Sec.С p.411-415.pdf | 777,9 kB | Adobe PDF | View/Open |
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