1,2,4-三唑-5- 1基苯磺酰胺的合成、生物活性和晶体结构

IF 4 2区 化学 Q2 CHEMISTRY, PHYSICAL
Kemal Sancak , Gülşah Gül Kılınç , Filiz Durak , Hanifi Özşanlı , Ufuk Çoruh , Burak Barut
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引用次数: 0

摘要

在本研究中,首先将肼羧酸酯(2)与3-(2氨基乙基)苯磺酰胺(1)在热控条件下进行环封闭反应,得到4-(2-(3-烷基/烷基芳基/芳基-5-氧-1,5-二氢- 4h -1,2,4-三唑-4-基)乙基)(3a-g)磺酰胺衍生物1,2,4-三唑-5- 1化合物。用FT-IR、1H-NMR和13C-NMR对合成的化合物进行了表征。第二步,对乙酰胆碱酯酶、丁基胆碱酯酶、α-糖苷酶和酪氨酸酶进行抑制实验,确定化合物的抑制特性。在对13种不同微生物的抗菌试验中,确定化合物对蜡状芽孢杆菌病原体有选择性有效。在部分研究中进行了抗氧化活性测试,除3a和3g外,所有化合物均具有中等自由基清除能力。通过XRD分析确定单晶(3d)的结构参数,揭示晶体结构信息。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

Synthesis, biological activities, and crystal structure of 1,2,4-triazole-5-one-based benzenesulfonamides

Synthesis, biological activities, and crystal structure of 1,2,4-triazole-5-one-based benzenesulfonamides
In this study, firstly the ring closed reaction of hydrazine carboxylates (2) with 3-(2 aminoethyl) benzene sulfonamide (1) in a thermally controlled reaction afforded 4-(2-(3-alkyl/alkylaryl/aryl-5-oxo-1,5-dihydro-4H-1,2,4-triazol-4-yl) ethyl) (3a-g) sulfonamide derivative 1,2,4-triazol-5-one compounds. The synthesized compounds were characterized using FT-IR, 1H-NMR and 13C-NMR spectra. In the second step, inhibition studies of acetylcholinesterase, butyrylcholinesterase α-glycosidase and tyrosinase were performed to determine the inhibitory properties of the compounds. In antimicrobial tests against 13 different microorganisms, it was determined that the compounds were selectively effective against the Bacillius Cereus pathogen. Antioxidant activity tests were performed in the part of the study, moderate radical scavenging properties were determined in all compounds except 3a and 3g. XRD analysis was performed to determine the structural parameters of the single crystal (3d) and to reveal the crystallographic structure information.
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来源期刊
Journal of Molecular Structure
Journal of Molecular Structure 化学-物理化学
CiteScore
7.10
自引率
15.80%
发文量
2384
审稿时长
45 days
期刊介绍: The Journal of Molecular Structure is dedicated to the publication of full-length articles and review papers, providing important new structural information on all types of chemical species including: • Stable and unstable molecules in all types of environments (vapour, molecular beam, liquid, solution, liquid crystal, solid state, matrix-isolated, surface-absorbed etc.) • Chemical intermediates • Molecules in excited states • Biological molecules • Polymers. The methods used may include any combination of spectroscopic and non-spectroscopic techniques, for example: • Infrared spectroscopy (mid, far, near) • Raman spectroscopy and non-linear Raman methods (CARS, etc.) • Electronic absorption spectroscopy • Optical rotatory dispersion and circular dichroism • Fluorescence and phosphorescence techniques • Electron spectroscopies (PES, XPS), EXAFS, etc. • Microwave spectroscopy • Electron diffraction • NMR and ESR spectroscopies • Mössbauer spectroscopy • X-ray crystallography • Charge Density Analyses • Computational Studies (supplementing experimental methods) We encourage publications combining theoretical and experimental approaches. The structural insights gained by the studies should be correlated with the properties, activity and/ or reactivity of the molecule under investigation and the relevance of this molecule and its implications should be discussed.
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