新的吡唑基四唑衍生物:合成、表征及其血管松弛和α-淀粉酶抑制活性

IF 3.3 4区 医学 Q2 BIOCHEMISTRY & MOLECULAR BIOLOGY
Ahlam Oulous, Ikram Dib, Tarik Harit, Abdullah Yahya Abdullah Alzahrani, Mounir Cherfi, Nour Elhouda Daoudi, Abderrahim Ziyyat, Fouad Malek
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引用次数: 0

摘要

合成了一系列新的线性吡唑基四唑衍生物1-10,并对其进行了表征。中间化合物的结构通过1H和13C NMR以及高分辨率质谱(HRMS)进行了确证。这些衍生物是通过吡唑和四唑前体之间的直接等摩尔缩合合成的。通过测定其抑制百分比E(%)来评估这些化合物的血管松弛活性,其范围从26%到67%,其中化合物4表现出最高的活性。此外,通过测定α-淀粉酶抑制的IC50值来评估其抗糖尿病潜能。值得注意的是,化合物2和6表现出与阳性对照阿卡波糖相当的活性。这些实验结果得到了分子对接研究的进一步支持。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
New Pyrazole-Based Tetrazole Derivatives: Synthesis, Characterization, and Their Vasorelaxant and α-Amylase Inhibition Activities

A series of new linear pyrazole-based tetrazole derivatives 110 were synthesized and characterized. The structures of the intermediate compounds were confirmed using 1H and 13C NMR spectroscopy, as well as high-resolution mass spectrometry (HRMS). These derivatives were synthesized through a straightforward equimolar condensation between pyrazole and tetrazole precursors. The vasorelaxant activity of these compounds was assessed by determining their percentage inhibition, E (%), which ranged from 26% to 67%, with compound 4 exhibiting the highest activity. Additionally, their anti-diabetic potential was evaluated by determining the IC50 values for α-amylase enzyme inhibition. Notably, compounds 2 and 6 demonstrated a comparable activity to the positive control acarbose. These experimental findings were further supported by molecular docking studies.

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来源期刊
Chemical Biology & Drug Design
Chemical Biology & Drug Design 医学-生化与分子生物学
CiteScore
5.10
自引率
3.30%
发文量
164
审稿时长
4.4 months
期刊介绍: Chemical Biology & Drug Design is a peer-reviewed scientific journal that is dedicated to the advancement of innovative science, technology and medicine with a focus on the multidisciplinary fields of chemical biology and drug design. It is the aim of Chemical Biology & Drug Design to capture significant research and drug discovery that highlights new concepts, insight and new findings within the scope of chemical biology and drug design.
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