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吡唑衍生物的合成及药理活性研究进展。

Synthesis and Pharmacological Activities of Pyrazole Derivatives: A Review.

机构信息

Medicinal Chemistry Laboratory, Faculty of Medicine and Pharmacy, Mohammed V University, 10100 Rabat, Morocco.

LCAE, Department of Chemistry, Faculty of Sciences, University Mohamed I, 60000 Oujda, Morocco.

出版信息

Molecules. 2018 Jan 12;23(1):134. doi: 10.3390/molecules23010134.

DOI:10.3390/molecules23010134
PMID:29329257
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC6017056/
Abstract

Pyrazole and its derivatives are considered a pharmacologically important active scaffold that possesses almost all types of pharmacological activities. The presence of this nucleus in pharmacological agents of diverse therapeutic categories such as celecoxib, a potent anti-inflammatory, the antipsychotic CDPPB, the anti-obesity drug rimonabant, difenamizole, an analgesic, betazole, a H2-receptor agonist and the antidepressant agent fezolamide have proved the pharmacological potential of the pyrazole moiety. Owing to this diversity in the biological field, this nucleus has attracted the attention of many researchers to study its skeleton chemically and biologically. This review highlights the different synthesis methods and the pharmacological properties of pyrazole derivatives. Studies on the synthesis and biological activity of pyrazole derivatives developed by many scientists around the globe are reported.

摘要

吡唑及其衍生物被认为是一种具有重要药理活性的基本结构,具有几乎所有类型的药理活性。在不同治疗类别的药物中都存在这个核,如塞来昔布(一种强效抗炎药)、CDPPB(一种抗精神病药)、利莫那班(一种减肥药)、地芬那酯(一种镇痛药)、贝他唑啉(一种 H2 受体激动剂)和非甾体类抗抑郁药 fezolamide,这证明了吡唑部分的药理潜力。由于其在生物领域的多样性,这个核已经吸引了许多研究人员从化学和生物学方面来研究其结构。本文综述了吡唑衍生物的不同合成方法和药理性质。报道了全球许多科学家对吡唑衍生物的合成和生物活性的研究。

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6
Design, Synthesis, and Characterization of Novel Pyrazole Cross-Linked Chitosan Derivatives Modified with Zinc Oxide Nanoparticles for Boosting Their Anticancer Activity.新型吡唑交联壳聚糖衍生物负载氧化锌纳米粒子的设计、合成与表征及其抗癌活性增强研究
Polymers (Basel). 2025 Apr 15;17(8):1061. doi: 10.3390/polym17081061.
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Synthesis, Anti-Inflammatory, and Molecular Docking Studies of New Heterocyclic Derivatives Comprising Pyrazole, Pyridine, and/or Pyran Moieties.含吡唑、吡啶和/或吡喃部分的新型杂环衍生物的合成、抗炎及分子对接研究
Pharmaceuticals (Basel). 2025 Feb 26;18(3):335. doi: 10.3390/ph18030335.
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Sulfonamide-Bearing Pyrazolone Derivatives as Multitarget Therapeutic Agents: Design, Synthesis, Characterization, Biological Evaluation, In Silico ADME/T Profiling and Molecular Docking Study.含磺酰胺基的吡唑啉酮衍生物作为多靶点治疗剂:设计、合成、表征、生物学评价、计算机辅助ADME/T分析及分子对接研究
Pharmacol Res Perspect. 2025 Apr;13(2):e70088. doi: 10.1002/prp2.70088.
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New pyrazole-based derivatives targeting MmpL3 transporter in Mycobacterium tuberculosis: design, synthesis, biological evaluation and molecular docking studies.新型靶向结核分枝杆菌MmpL3转运蛋白的吡唑基衍生物:设计、合成、生物学评价及分子对接研究
Mol Divers. 2025 Mar 14. doi: 10.1007/s11030-025-11152-3.
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The synthesis and investigation of novel 3-benzoylbenzofurans and pyrazole derivatives for anti-HIV activity.新型3-苯甲酰基苯并呋喃和吡唑衍生物的合成及其抗HIV活性研究
RSC Med Chem. 2025 Feb 5;16(5):2142-2158. doi: 10.1039/d4md00844h. eCollection 2025 May 22.
吡唑基三唑类化合物作为抗菌和抗炎剂的合成、药理活性及分子对接研究
Bioorg Med Chem. 2017 Oct 15;25(20):5678-5691. doi: 10.1016/j.bmc.2017.08.042. Epub 2017 Sep 15.
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Design, synthesis and antitumor activity of Novel Sorafenib derivatives bearing pyrazole scaffold.含吡唑骨架的新型索拉非尼衍生物的设计、合成及抗肿瘤活性
Bioorg Med Chem. 2017 Oct 15;25(20):5754-5763. doi: 10.1016/j.bmc.2017.09.003. Epub 2017 Sep 6.
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Pyrazole-based compounds in chitosan liposomal emulsion for antimicrobial cotton fabrics.壳聚糖脂质体乳液中吡唑类化合物在抗菌棉织物中的应用。
Int J Biol Macromol. 2018 Feb;107(Pt A):585-594. doi: 10.1016/j.ijbiomac.2017.09.031. Epub 2017 Sep 13.
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In vitro genotoxicity and in vivo subchronic evaluation of the anti-inflammatory pyrazole compound LQFM021.抗炎吡唑化合物 LQFM021 的体外遗传毒性和体内亚慢性评价。
Chem Biol Interact. 2017 Nov 1;277:185-194. doi: 10.1016/j.cbi.2017.09.004. Epub 2017 Sep 7.
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Pyrazole-hydrazone derivatives as anti-inflammatory agents: Design, synthesis, biological evaluation, COX-1,2/5-LOX inhibition and docking study.吡唑腙衍生物作为抗炎剂:设计、合成、生物学评价、COX-1、2/5-LOX抑制及对接研究
Bioorg Chem. 2017 Oct;74:212-220. doi: 10.1016/j.bioorg.2017.08.014. Epub 2017 Aug 30.
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Synthesis, antimycobacterial activity and docking study of 2-aroyl-[1]benzopyrano[4,3-c]pyrazol-4(1H)-one derivatives and related hydrazide-hydrazones.2-芳酰基-[1]苯并吡喃并[4,3-c]吡唑-4(1H)-酮衍生物及相关酰肼腙的合成、抗分枝杆菌活性与对接研究
Bioorg Med Chem Lett. 2017 Jul 1;27(13):2996-3002. doi: 10.1016/j.bmcl.2017.05.011. Epub 2017 May 5.
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Part I: Design, synthesis and biological evaluation of novel pyrazole-benzimidazole conjugates as checkpoint kinase 2 (Chk2) inhibitors with studying their activities alone and in combination with genotoxic drugs.第一部分:新型吡唑-苯并咪唑偶联物作为细胞周期检查点激酶 2(Chk2)抑制剂的设计、合成与生物评价,研究其单独及与遗传毒性药物联合应用的活性。
Eur J Med Chem. 2017 Jul 7;134:392-405. doi: 10.1016/j.ejmech.2017.03.090. Epub 2017 Apr 14.
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Simple dialkyl pyrazole-3,5-dicarboxylates show in vitro and in vivo activity against disease-causing trypanosomatids.简单的二烷基吡唑-3,5-二羧酸酯在体外和体内对致病锥虫显示出活性。
Parasitology. 2017 Aug;144(9):1133-1143. doi: 10.1017/S0031182017000415. Epub 2017 Apr 3.