Suppr超能文献

[3-芳基-4-氨基-5-巯基-4H-1,2,4-三唑的反应活性:7H-1,2,4-噻唑并[3,4-b][1,3,4]噻二嗪的3,6-二芳基衍生物、3-芳基-4-氨基-5-羧甲基硫基-4H-1,2,4-三唑的合成与生物学评价]

[Reactivity of 3-aryl-4-amino-5-mercapto-4H-1,2,4-triazoles: synthesis and biological evaluation of 3,6-diaryl derivatives of 7H-1,2,4-thiazole[3,4-b][1,3,4]thiadiazines, of 3-aryl-4-amino-5-carboxymethylthio-4H-1,2,4-triazoles].

作者信息

Mazzone G, Bonina F, Panico A M, Amico-Roxas M, Caruso A, Blandino G, Vanella A

机构信息

Istituto di Chimica Farmaceutica e Tossicologica dell'Università di Catania.

出版信息

Farmaco Sci. 1987 Jul;42(7):525-39.

PMID:2822474
Abstract

Starting from 3-aryl-4-amino-5-mercapto-4H-1,2,4-triazoles (II), two series of 3,6-disubstituted 7H-1,2,4-triazol [3,4-b] [1,3,4] thiadiazines (III) and their 5-carboxymethylthio derivatives (IV) were prepared. From the mercapto-amino-triazoles (II) because of their reactivity in some oxidising media, were obtained the triazole derivatives (V), (VI) and (VII). The synthesis of the alpha-thioketones (VIII) of 3-aryl-5-mercapto-1,3,4-oxadiazoles (I), used in alternative synthesis of triazole-thiadiazines (III), is also reported. All the substances described were subjected to biological screening. In the tests, the carboxymethylthiotriazole (IV) showed weak antiinflammatory activity (carrageenin edema) and more consistent scavanger activity, in vitro, on superoxide anions. The triazole-thiadiazines (III) and triazoles (II), (V) and (VI) showed moderate antimycotic activity.

摘要

从3-芳基-4-氨基-5-巯基-4H-1,2,4-三唑(II)出发,制备了两个系列的3,6-二取代的7H-1,2,4-三唑并[3,4-b][1,3,4]噻二嗪(III)及其5-羧甲基硫代衍生物(IV)。由于巯基氨基三唑(II)在某些氧化介质中的反应活性,得到了三唑衍生物(V)、(VI)和(VII)。还报道了用于三唑并噻二嗪(III)的替代合成的3-芳基-5-巯基-1,3,4-恶二唑(I)的α-硫酮(VIII)的合成。对所描述的所有物质进行了生物筛选。在试验中,羧甲基硫代三唑(IV)表现出较弱的抗炎活性(角叉菜胶性水肿),并且在体外对超氧阴离子具有更稳定的清除活性。三唑并噻二嗪(III)以及三唑(II)、(V)和(VI)表现出中等的抗真菌活性。

文献检索

告别复杂PubMed语法,用中文像聊天一样搜索,搜遍4000万医学文献。AI智能推荐,让科研检索更轻松。

立即免费搜索

文件翻译

保留排版,准确专业,支持PDF/Word/PPT等文件格式,支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述,25分钟生成高质量综述,智能提取关键信息,辅助科研写作。

立即免费体验