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本文引用的文献

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Synthesis of pyrazino[1,2-]indazoles cascade cyclization of indazole aldehydes with propargylic amines.吡嗪并[1,2 - ]吲唑的合成:吲唑醛与炔丙胺的串联环化反应。
Org Biomol Chem. 2024 Mar 13;22(11):2226-2230. doi: 10.1039/d4ob00051j.
2
Evaluation of the Indazole Analogs of 5-MeO-DMT and Related Tryptamines as Serotonin Receptor 2 Agonists.5-甲氧基-N,N-二甲基色胺及其相关色胺的吲唑类似物作为5-羟色胺受体2激动剂的评估
ACS Med Chem Lett. 2024 Jan 19;15(2):302-309. doi: 10.1021/acsmedchemlett.3c00566. eCollection 2024 Feb 8.
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Synthesis of Indazoles via N-N Bond-Forming Oxidative Cyclization from 2-Aminomethyl-phenylamines.通过2-氨基甲基苯胺的N-N键形成氧化环化反应合成吲唑类化合物。
Org Lett. 2024 Feb 16;26(6):1229-1232. doi: 10.1021/acs.orglett.4c00036. Epub 2024 Feb 5.
4
Design, synthesis, and pharmacological evaluation of indazole carboxamides of N-substituted pyrrole derivatives as soybean lipoxygenase inhibitors.N-取代吡咯衍生物的吲唑甲酰胺类化合物作为大豆脂氧合酶抑制剂的设计、合成及药理评价
Mol Divers. 2024 Dec;28(6):3757-3782. doi: 10.1007/s11030-023-10775-8. Epub 2023 Dec 25.
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Identification of Indazole-Based Thiadiazole-Bearing Thiazolidinone Hybrid Derivatives: Theoretical and Computational Approaches to Develop Promising Anti-Alzheimer's Candidates.含吲唑基噻二唑的噻唑烷酮杂化衍生物的鉴定:开发有前景的抗阿尔茨海默病候选药物的理论与计算方法
Pharmaceuticals (Basel). 2023 Nov 30;16(12):1667. doi: 10.3390/ph16121667.
6
Liposomal formulation of a new antifungal hybrid compound provides protection against in the skin colonization model.新型抗真菌杂合化合物的脂质体制剂为 皮肤定植模型提供保护。
Antimicrob Agents Chemother. 2024 Jan 10;68(1):e0095523. doi: 10.1128/aac.00955-23. Epub 2023 Dec 11.
7
Discovery of novel 3-(1H-pyrazol-4-yl)-1H-indazole derivatives as potent type II TRK inhibitors against acquired resistance.发现新型 3-(1H-吡唑-4-基)-1H-吲唑衍生物作为有效的 II 型 TRK 抑制剂,可对抗获得性耐药。
Eur J Med Chem. 2024 Jan 15;264:115953. doi: 10.1016/j.ejmech.2023.115953. Epub 2023 Nov 15.
8
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J Med Chem. 2023 Nov 23;66(22):15205-15229. doi: 10.1021/acs.jmedchem.3c01297. Epub 2023 Nov 9.
9
Synthesis and Staphylococcus aureus biofilm inhibitory activity of indolenine-substituted pyrazole and pyrimido[1,2-b]indazole derivatives.吲哚啉取代的吡唑和嘧啶并[1,2-b]吲哚衍生物的合成及其对金黄色葡萄球菌生物膜的抑制活性
Bioorg Med Chem. 2023 Nov 15;95:117485. doi: 10.1016/j.bmc.2023.117485. Epub 2023 Sep 30.
10
Indazole as a Phenol Bioisostere: Structure-Affinity Relationships of GluN2B-Selective NMDA Receptor Antagonists.吲唑作为酚类生物等排体:GluN2B 选择性 NMDA 受体拮抗剂的结构-亲和力关系。
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吲唑——一种新兴的优势骨架:合成及其生物学意义

Indazole - an emerging privileged scaffold: synthesis and its biological significance.

作者信息

Singampalli Anuradha, Kumar Pardeep, Bandela Rani, Bellapukonda Sri Mounika, Nanduri Srinivas, Yaddanapudi Venkata Madhavi

机构信息

Department of Chemical Sciences, National Institute of Pharmaceutical Education and Research (NIPER) Hyderabad 500037 India

出版信息

RSC Med Chem. 2025 Aug 19. doi: 10.1039/d5md00336a.

DOI:10.1039/d5md00336a
PMID:40937103
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC12421766/
Abstract

Nitrogen-containing molecules are an important class of heterocyclic compounds. Among these, indazole is one of the most important scaffolds with a broad scope because of its pharmaceutical and biological properties. Many novel molecules were reported in clinical trials for treating various diseases containing the indazole scaffold. Indazole has a vast potential for the discovery of novel pharmaceuticals such as anti-bacterial, anti-fungal, anti-leishmanial, antidiabetic, anti-cancer, anti-tuberculosis, anti-Parkinson's, anti-protozoal, anti-depressant, and anti-inflammatory. This review covers the structures of new indazoles, the current pipeline of indazole-containing compounds in the various stages of clinical trials, and naturally occurring indazoles, along with some marketed drugs. Furthermore, we have covered the different methods for the synthesis of 1-indazole, 2-indazole, and 3-indazole with a wide variety of starting materials under different reaction conditions and their biological activities.

摘要

含氮分子是一类重要的杂环化合物。其中,吲唑是最重要的骨架之一,因其具有药物和生物学特性而具有广泛的应用范围。许多含有吲唑骨架的新型分子已在治疗各种疾病的临床试验中被报道。吲唑在发现新型药物方面具有巨大潜力,如抗菌、抗真菌、抗利什曼原虫、抗糖尿病、抗癌、抗结核、抗帕金森病、抗原虫、抗抑郁和抗炎药物。本综述涵盖了新型吲唑的结构、处于临床试验各阶段的含吲唑化合物的当前研发情况、天然存在的吲唑以及一些上市药物。此外,我们还介绍了在不同反应条件下使用多种起始原料合成1-吲唑、2-吲唑和3-吲唑的不同方法及其生物活性。