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吡唑并[5,1-][1,2,4]三唑：药物化学中一种有前景的新兴生物活性骨架。

Pyrazolo[5,1-][1,2,4]triazole: A Promising Emerging Biologically Active Scaffold in Medicinal Chemistry.

作者信息

Pintea Beniamin-Nicolae, Panțîr Vasilica-Georgiana, Badea Valentin, Péter Francisc

机构信息

Department of Applied Chemistry and Engineering of Organic and Natural Compounds, Faculty of Chemical Engineering, Biotechnology, and Environmental Protection, University Politehnica Timișoara, Vasile Parvan Blv. 6, 300223 Timișoara, Romania.

出版信息

Int J Mol Sci. 2025 Aug 23;26(17):8190. doi: 10.3390/ijms26178190.

DOI:10.3390/ijms26178190
PMID:40943116
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC12427664/
Abstract

Nitrogen-containing heterocycles are essential compounds in nature, and their structural and functional diversity inspired the synthesis of a wide range of derivatives with diverse applications as pharmaceuticals, agrochemicals, dyes, polymers, cosmetics, etc. Among them, -fused heterocycles represent an important category, due to their high potential as biologically active agents. Pyrazolo[5,1-][1,2,4]triazoles, a class of nitrogen heterobicycles, have multiple applications as dyes and pigments. Also, a number of compounds containing this structure have been investigated for their biological activities. All the main experimental results published in the literature (both articles and patents) regarding the latter are summarized in this review.

摘要

含氮杂环是自然界中的重要化合物，其结构和功能的多样性激发了人们合成各种衍生物的灵感，这些衍生物在药物、农用化学品、染料、聚合物、化妆品等领域有着广泛的应用。其中，稠合杂环因其作为生物活性剂的巨大潜力而成为一个重要类别。吡唑并[5,1 - ][1,2,4]三唑是一类氮杂双环化合物，作为染料和颜料有多种应用。此外，许多含有这种结构的化合物已被研究其生物活性。本文综述了文献（包括文章和专利）中发表的关于后者的所有主要实验结果。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5a8d/12427664/70b9fb38b76d/ijms-26-08190-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5a8d/12427664/bfbd40e2266f/ijms-26-08190-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5a8d/12427664/20f979778201/ijms-26-08190-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5a8d/12427664/95f49c77afd1/ijms-26-08190-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5a8d/12427664/4bb021bd8518/ijms-26-08190-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5a8d/12427664/70b9fb38b76d/ijms-26-08190-g005.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5a8d/12427664/bfbd40e2266f/ijms-26-08190-g001.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5a8d/12427664/20f979778201/ijms-26-08190-g002.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5a8d/12427664/95f49c77afd1/ijms-26-08190-g003.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5a8d/12427664/4bb021bd8518/ijms-26-08190-g004.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/5a8d/12427664/70b9fb38b76d/ijms-26-08190-g005.jpg

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本文引用的文献

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Chem Biodivers. 2025 Aug;22(8):e202500260. doi: 10.1002/cbdv.202500260. Epub 2025 Mar 27.
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Utility of sulfachloropyridazine in the synthesis of novel anticancer agents as antiangiogenic and apoptotic inducers.磺胺氯哒嗪在新型抗癌剂合成中的应用，作为抗血管生成和诱导凋亡的试剂。
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Anticancer evaluation and molecular docking of new pyridopyrazolo-triazine and pyridopyrazolo-triazole derivatives.
新型吡啶并吡唑三嗪和吡啶并吡唑三唑衍生物的抗癌评价及分子对接。
Sci Rep. 2023 Feb 16;13(1):2782. doi: 10.1038/s41598-023-29908-y.
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An Overview of the Biological Evaluation of Selected Nitrogen-Containing Heterocycle Medicinal Chemistry Compounds.含氮杂环类药物化学化合物的生物评价概述。
Int J Mol Sci. 2022 Jul 23;23(15):8117. doi: 10.3390/ijms23158117.
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Rapid syntheses of N-fused heterocycles via acyl-transfer in heteroaryl ketones.通过杂芳基酮中的酰基转移快速合成 N-稠合杂环。
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Structure-Activity Relationship of Phenylpyrazolones against Trypanosoma cruzi.苯骈吡唑酮类化合物抗克氏锥虫的构效关系。
ChemMedChem. 2020 Jul 20;15(14):1310-1321. doi: 10.1002/cmdc.202000136. Epub 2020 Apr 27.
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Synthesis, biological activity and molecular modeling of a new series of condensed 1,2,4-triazoles.缩合 1,2,4-三唑类新系列的合成、生物活性及分子模拟。
Bioorg Chem. 2019 Nov;92:103193. doi: 10.1016/j.bioorg.2019.103193. Epub 2019 Aug 12.
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