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新型4H-1,4-苯并噻嗪及其砜类似物和呋喃核糖苷的合成、光谱表征及药理学重要性

Synthesis, spectral characterization, and pharmacological importance of new 4H-1,4-benzothiazines, their sulfone analogues, and ribofuranosides.

作者信息

Gautam Naveen, Garg Ankita, Gautam Dinesh Chand

机构信息

a Lal Bahadur Shastri Government P.G. College, Kotputli , Jaipur , Rajasthan , India.

出版信息

Nucleosides Nucleotides Nucleic Acids. 2015;34(1):40-55. doi: 10.1080/15257770.2014.955194.

Abstract

The present article describes the synthesis of new 4H-1,4-benzothiazines via condensation and oxidative cyclization of substituted 2-aminobenzenethiols with compounds containing active methylene groups. It is believed that the reaction proceeds via intermediary of the enaminoketone system. The sulfone derivatives were synthesized by oxidation of 4H-1,4-benzothiazines using 30% hydrogen peroxide in glacial acetic acid. Benzothiazines were used as bases to prepare ribofuranosides by treatment with a sugar derivative (β-D-ribofuranosyl-1-acetate-2,3,5-tribenzoate). The pharmacological importance of the synthesized compounds was evaluated by their, antimicrobial properties against various bacterial strains and fungal species. The structures of the compounds have been confirmed by spectral and chemical analysis.

摘要

本文描述了通过取代的2-氨基苯硫醇与含活性亚甲基的化合物进行缩合和氧化环化反应合成新型4H-1,4-苯并噻嗪的方法。据信该反应通过烯胺酮体系作为中间体进行。使用30%的过氧化氢在冰醋酸中氧化4H-1,4-苯并噻嗪合成砜衍生物。苯并噻嗪用作碱,通过与糖衍生物(β-D-呋喃核糖基-1-乙酸酯-2,3,5-三苯甲酸酯)反应制备呋喃核糖苷。通过所合成化合物对各种细菌菌株和真菌物种的抗菌性能评估了其药理学重要性。化合物的结构已通过光谱和化学分析得到证实。

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