• 文献检索
  • 文档翻译
  • 深度研究
  • 学术资讯
  • Suppr Zotero 插件Zotero 插件
  • 邀请有礼
  • 套餐&价格
  • 历史记录
应用&插件
Suppr Zotero 插件Zotero 插件浏览器插件Mac 客户端Windows 客户端微信小程序
定价
高级版会员购买积分包购买API积分包
服务
文献检索文档翻译深度研究API 文档MCP 服务
关于我们
关于 Suppr公司介绍联系我们用户协议隐私条款
关注我们

Suppr 超能文献

核心技术专利:CN118964589B侵权必究
粤ICP备2023148730 号-1Suppr @ 2026

文献检索

告别复杂PubMed语法,用中文像聊天一样搜索,搜遍4000万医学文献。AI智能推荐,让科研检索更轻松。

立即免费搜索

文件翻译

保留排版,准确专业,支持PDF/Word/PPT等文件格式,支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述,25分钟生成高质量综述,智能提取关键信息,辅助科研写作。

立即免费体验

吡唑啉及相关衍生物的合成方法、生物活性及构效关系。

Synthetic Approaches, Biological Activities, and Structure-Activity Relationship of Pyrazolines and Related Derivatives.

机构信息

Department of Pharmaceutical Chemistry, Noida Institute of Engineering and Technology (Pharmacy Institute), Greater Noida, India.

出版信息

Top Curr Chem (Cham). 2023 Apr 8;381(3):12. doi: 10.1007/s41061-023-00422-z.

DOI:10.1007/s41061-023-00422-z
PMID:37029841
Abstract

It has been established that pyrazolines and their analogs are pharmacologically active scaffolds. The pyrazoline moiety is present in several marketed molecules with a wide range of uses, which has established its importance in pharmaceutical and agricultural sectors, as well as in industry. Due to its broad-spectrum utility, scientists are continuously captivated by pyrazolines and their derivatives to study their chemistry. Pyrazolines or their analogs can be prepared by several synthesis strategies, and the focus will always be on new greener and more economical ways for their synthesis. Among these methods, chalcones, hydrazines, diazo compounds, and hydrazones are most commonly applied under different reaction conditions for the synthesis of pyrazoline and its analogs. However, there is scope for other molecules such as Huisgen zwitterions, different metal catalysts, and nitrile imine to be used as starting reagents. The present article consists of recently reported synthetic protocols, pharmacological activities, and the structure-activity relationship of pyrazoline and its derivatives, which will be very useful to researchers.

摘要

已经证实,吡唑啉及其类似物是具有药理活性的支架。吡唑啉部分存在于多种具有广泛用途的市售分子中,这使其在制药和农业以及工业领域都具有重要地位。由于其广谱用途,科学家们一直对吡唑啉及其衍生物着迷,以研究它们的化学性质。吡唑啉或其类似物可以通过几种合成策略来制备,而重点始终是寻找新的、更绿色、更经济的合成方法。在这些方法中,查尔酮、肼、重氮化合物和腙最常用于不同的反应条件下合成吡唑啉及其类似物。然而,其他分子如 Huisgen 两性离子、不同的金属催化剂和腈亚胺也可以用作起始试剂。本文包含了最近报道的吡唑啉及其衍生物的合成方案、药理学活性和构效关系,这对研究人员将非常有用。

相似文献

1
Synthetic Approaches, Biological Activities, and Structure-Activity Relationship of Pyrazolines and Related Derivatives.吡唑啉及相关衍生物的合成方法、生物活性及构效关系。
Top Curr Chem (Cham). 2023 Apr 8;381(3):12. doi: 10.1007/s41061-023-00422-z.
2
Pyrazoline and Analogs: Substrate-based Synthetic Strategies.吡唑啉及其类似物:基于底物的合成策略。
Curr Org Synth. 2024;21(7):823-836. doi: 10.2174/1570179421666230822100043.
3
Recent Updates on Pyrazoline Derivatives as Promising Candidates for Neuropsychiatric and Neurodegenerative Disorders.吡唑啉衍生物作为神经精神和神经退行性疾病有希望的候选药物的最新进展。
Curr Top Med Chem. 2021;21(30):2695-2714. doi: 10.2174/1568026621999210902123132.
4
Synthesis of novel analogs of 2-pyrazoline obtained from [(7-chloroquinolin-4-yl)amino]chalcones and hydrazine as potential antitumor and antimalarial agents.合成新型 2-吡唑啉类似物,该类似物由[(7-氯喹啉-4-基)氨基]查耳酮和肼反应得到,作为潜在的抗肿瘤和抗疟药物。
Eur J Med Chem. 2013 Sep;67:252-62. doi: 10.1016/j.ejmech.2013.06.049. Epub 2013 Jul 2.
5
Synthesis and DFT Calculations of Novel Vanillin-Chalcones and Their 3-Aryl-5-(4-(2-(dimethylamino)-ethoxy)-3-methoxyphenyl)-4,5-dihydro-1H-pyrazole-1-carbaldehyde Derivatives as Antifungal Agents.新型香草基查耳酮及其 3-芳基-5-(4-(2-(二甲氨基)乙氧基)-3-甲氧基苯基)-4,5-二氢-1H-吡唑-1-甲酰衍生物的合成及 DFT 计算作为抗真菌剂。
Molecules. 2017 Sep 5;22(9):1476. doi: 10.3390/molecules22091476.
6
An efficient synthesis of new caffeine-based chalcones, pyrazolines and pyrazolo[3,4-b][1,4]diazepines as potential antimalarial, antitrypanosomal and antileishmanial agents.新型咖啡因基查耳酮、吡唑啉和吡唑并[3,4-b][1,4]二氮杂卓作为潜在抗疟、抗锥虫和抗利什曼原虫药物的高效合成。
Eur J Med Chem. 2015 Mar 26;93:401-13. doi: 10.1016/j.ejmech.2015.02.040. Epub 2015 Feb 21.
7
Synthesis, Cytotoxicity Evaluation, Molecular Docking and Utility of Novel Chalcones as Precursors for Heterocycles Incorporating Pyrazole Moiety.新型查尔酮作为含吡唑部分杂环前体的合成、细胞毒性评估、分子对接及应用
Med Chem. 2018;14(4):344-355. doi: 10.2174/1573406413666171020114105.
8
Synthesis, in vitro antibacterial and antifungal activity of some n-acetylated and non-acetylated pyrazolines.某些N-乙酰化和非乙酰化吡唑啉的合成、体外抗菌和抗真菌活性
Pak J Pharm Sci. 2013 Jan;26(1):67-73.
9
Reactions of hydroxybenzofurans. VI. Syntheses of benzofuran chalcones, hydrazones and pyrazolines of potential biological activity.羟基苯并呋喃的反应。VI. 具有潜在生物活性的苯并呋喃查耳酮、腙和吡唑啉的合成。
Arzneimittelforschung. 1977;27(11):2035-8.
10
SAR studies of differently functionalized chalcones based hydrazones and their cyclized derivatives as inhibitors of mammalian cathepsin B and cathepsin H.基于查耳酮的不同功能化腙及其环化衍生物作为哺乳动物组织蛋白酶B和组织蛋白酶H抑制剂的构效关系研究
Bioorg Med Chem. 2014 Aug 1;22(15):4233-45. doi: 10.1016/j.bmc.2014.05.037. Epub 2014 May 24.

引用本文的文献

1
Unveiling the migration reactivity of bicyclic diaziridines: enantioselective synthesis of chiral pyrazolines.揭示双环二氮丙啶的迁移反应活性:手性吡唑啉的对映选择性合成
Chem Sci. 2025 Aug 11. doi: 10.1039/d5sc04846j.
2
Discovery of 2-Pyrazolines That Inhibit the Phosphorylation of STAT3 as Nanomolar Cytotoxic Agents.发现作为纳摩尔细胞毒性剂抑制信号转导和转录激活因子3(STAT3)磷酸化的2-吡唑啉类化合物。
ACS Omega. 2025 Jan 2;10(1):114-126. doi: 10.1021/acsomega.3c10504. eCollection 2025 Jan 14.
3
Exploring pyrazolines as potential inhibitors of NSP3-macrodomain of SARS-CoV-2: synthesis and in silico analysis.

本文引用的文献

1
Synthesis of pyrazoline fatty chain derivatives and its effects on melanoma cells.吡唑啉脂肪链衍生物的合成及其对黑素瘤细胞的影响。
Bioorg Med Chem Lett. 2021 Jun 1;41:127988. doi: 10.1016/j.bmcl.2021.127988. Epub 2021 Mar 26.
2
Copper-Catalyzed Aerobic Cyclization of β,γ-Unsaturated Hydrazones with Concomitant C═C Bond Cleavage.铜催化β,γ-不饱和腙的需氧环化反应及伴随的碳-碳双键断裂
Org Lett. 2020 Oct 16;22(20):7981-7985. doi: 10.1021/acs.orglett.0c02911. Epub 2020 Oct 6.
3
A One-Step Approach to -(Hetero)aryl-3,5-dinitropyrazoles from (Hetero)aryl Amines.
探索吡唑啉作为新型冠状病毒NSP3-巨结构域潜在抑制剂:合成与计算机模拟分析
Sci Rep. 2025 Jan 4;15(1):767. doi: 10.1038/s41598-024-81711-5.
4
Catalytic enantioselective synthesis of 2-pyrazolines one-pot condensation/6π-electrocyclization: 3,5-bis(pentafluorosulfanyl)-phenylthioureas as powerful hydrogen bond donors.2-吡唑啉的催化对映选择性合成——一锅法缩合/6π-电环化反应:3,5-双(五氟硫烷基)-苯基硫脲作为强效氢键供体
Chem Sci. 2024 Aug 26;15(37):15456-62. doi: 10.1039/d4sc04760e.
一种从(杂)芳基胺制备 -(杂)芳基-3,5-二硝基吡唑的一步法
Org Lett. 2020 Aug 7;22(15):5866-5869. doi: 10.1021/acs.orglett.0c01960. Epub 2020 Jul 16.
4
Overview of recent developments of pyrazole derivatives as an anticancer agent in different cell line.吡唑衍生物作为一种抗癌剂在不同细胞系中的最新发展概述。
Bioorg Chem. 2020 Apr;97:103470. doi: 10.1016/j.bioorg.2019.103470. Epub 2019 Dec 14.
5
Regioselective Synthesis of 3-Trifluoromethylpyrazole by Coupling of Aldehydes, Sulfonyl Hydrazides, and 2-Bromo-3,3,3-trifluoropropene.醛、亚磺酰肼和 2-溴-3,3,3-三氟丙烯的区域选择性合成 3-三氟甲基吡唑。
Org Lett. 2020 Feb 7;22(3):809-813. doi: 10.1021/acs.orglett.9b04228. Epub 2020 Jan 17.
6
Copper(I)-Catalyzed Oxyamination of β,γ-Unsaturated Hydrazones: Synthesis of Dihydropyrazoles.铜(I)催化的β,γ-不饱和腙的加氧氨化反应:二氢吡唑的合成。
Org Lett. 2019 Oct 4;21(19):7787-7790. doi: 10.1021/acs.orglett.9b02733. Epub 2019 Sep 20.
7
Design, synthesis, modeling studies and biological screening of novel pyrazole derivatives as potential analgesic and anti-inflammatory agents.设计、合成、建模研究及新型吡唑衍生物的生物筛选,作为有潜力的镇痛和抗炎药物。
Bioorg Chem. 2019 Aug;89:103023. doi: 10.1016/j.bioorg.2019.103023. Epub 2019 May 31.
8
The Divergent Effects of CDPPB and Cannabidiol on Fear Extinction and Anxiety in a Predator Scent Stress Model of PTSD in Rats.CDPPB和大麻二酚对大鼠创伤后应激障碍捕食者气味应激模型中恐惧消退和焦虑的不同影响
Front Behav Neurosci. 2019 May 10;13:91. doi: 10.3389/fnbeh.2019.00091. eCollection 2019.
9
Copper-Catalyzed Aminoboration from Hydrazones To Generate Borylated Pyrazoles.铜催化腙的氨基硼化反应以生成硼化吡唑。
Org Lett. 2019 Mar 1;21(5):1283-1286. doi: 10.1021/acs.orglett.8b04038. Epub 2019 Feb 12.
10
Synthesis, Biological Evaluation and Molecular Docking Studies of New Pyrazolines as an Antitubercular and Cytotoxic Agents.新型吡唑啉类抗结核和细胞毒性药物的合成、生物学评价及分子对接研究
Infect Disord Drug Targets. 2019;19(3):310-321. doi: 10.2174/1871526519666181217120626.