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Structure-activity relationship of pyrrolyl diketo acid derivatives as dual inhibitors of HIV-1 integrase and reverse transcriptase ribonuclease H domain.吡咯二酮酸衍生物作为 HIV-1 整合酶和逆转录酶核糖核酸酶 H 结构域双重抑制剂的构效关系。
J Med Chem. 2015 Feb 26;58(4):1915-28. doi: 10.1021/jm501799k. Epub 2015 Feb 11.
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5-Hydroxypyrido[2,3-b]pyrazin-6(5H)-one derivatives as novel dual inhibitors of HIV-1 reverse transcriptase-associated ribonuclease H and integrase.5-羟吡啶并[2,3-b]吡嗪-6(5H)-酮衍生物作为新型 HIV-1 逆转录酶相关核糖核酸酶 H 和整合酶双重抑制剂。
Eur J Med Chem. 2018 Jul 15;155:714-724. doi: 10.1016/j.ejmech.2018.06.036. Epub 2018 Jun 18.
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Molecular Docking and Molecular Dynamics Simulation Based Approach to Explore the Dual Inhibitor Against HIV-1 Reverse Transcriptase and Integrase.基于分子对接和分子动力学模拟的方法探索抗HIV-1逆转录酶和整合酶的双重抑制剂
Comb Chem High Throughput Screen. 2017;20(8):734-746. doi: 10.2174/1386207320666170615104703.
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New insights into the interaction between pyrrolyl diketoacids and HIV-1 integrase active site and comparison with RNase H.吡咯基二酮酸与HIV-1整合酶活性位点相互作用的新见解及与核糖核酸酶H的比较。
Antiviral Res. 2016 Oct;134:236-243. doi: 10.1016/j.antiviral.2016.09.008. Epub 2016 Sep 20.
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Diketo acids derivatives as dual inhibitors of human immunodeficiency virus type 1 integrase and the reverse transcriptase RNase H domain.二酮酸衍生物作为人类免疫缺陷病毒 1 型整合酶和逆转录酶 RNase H 结构域的双重抑制剂。
Curr Med Chem. 2011;18(22):3335-42. doi: 10.2174/092986711796504619.
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Design and synthesis of dual inhibitors of HIV reverse transcriptase and integrase: introducing a diketoacid functionality into delavirdine.HIV逆转录酶和整合酶双重抑制剂的设计与合成：将二酮酸官能团引入地拉韦啶
Bioorg Med Chem. 2008 Apr 1;16(7):3587-95. doi: 10.1016/j.bmc.2008.02.007. Epub 2008 Feb 8.
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6-(1-Benzyl-1H-pyrrol-2-yl)-2,4-dioxo-5-hexenoic acids as dual inhibitors of recombinant HIV-1 integrase and ribonuclease H, synthesized by a parallel synthesis approach.6-(1-苄基-1H-吡咯-2-基)-2,4-二氧代-5-己烯酸作为重组 HIV-1 整合酶和核糖核酸酶 H 的双重抑制剂，通过平行合成方法合成。
J Med Chem. 2013 Nov 14;56(21):8588-98. doi: 10.1021/jm401040b. Epub 2013 Nov 5.
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Past and future. Current drugs targeting HIV-1 integrase and reverse transcriptase-associated ribonuclease H activity: single and dual active site inhibitors.过去与未来。目前针对HIV-1整合酶和逆转录酶相关核糖核酸酶H活性的药物：单活性位点和双活性位点抑制剂。
Antivir Chem Chemother. 2014 Jan 29;23(4):129-44. doi: 10.3851/IMP2690.
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Prediction of the binding mode and resistance profile for a dual-target pyrrolyl diketo acid scaffold against HIV-1 integrase and reverse-transcriptase-associated ribonuclease H.预测针对 HIV-1 整合酶和逆转录酶相关核糖核酸酶 H 的双靶吡咯二酮酸支架的结合模式和耐药谱。
Phys Chem Chem Phys. 2018 Sep 26;20(37):23873-23884. doi: 10.1039/c8cp01843j.
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Pharmacophore and structure-activity relationships of integrase inhibition within a dual inhibitor scaffold of HIV reverse transcriptase and integrase.HIV 逆转录酶和整合酶双重抑制剂骨架内整合酶抑制作用的药效团和结构活性关系。
Bioorg Med Chem. 2010 Jun 15;18(12):4202-11. doi: 10.1016/j.bmc.2010.05.004. Epub 2010 May 7.
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Exploring structure-activity relationships of pyrrolyl diketo acid derivatives as non-nucleoside inhibitors of terminal deoxynucleotidyl transferase enzyme.探索吡咯基二酮酸衍生物作为末端脱氧核苷酸转移酶非核苷抑制剂的构效关系。
J Enzyme Inhib Med Chem. 2025 Dec;40(1):2496782. doi: 10.1080/14756366.2025.2496782. Epub 2025 Jun 9.
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Quinolinonyl Derivatives as Dual Inhibitors of the HIV-1 Integrase Catalytic Site and Integrase-RNA interactions.喹啉基衍生物作为HIV-1整合酶催化位点和整合酶-RNA相互作用的双重抑制剂
ACS Med Chem Lett. 2024 Aug 5;15(9):1533-1540. doi: 10.1021/acsmedchemlett.4c00268. eCollection 2024 Sep 12.
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Targeting Ribonucleases with Small Molecules and Bifunctional Molecules.靶向核糖核酸酶的小分子和双功能分子。
ACS Chem Biol. 2023 Oct 20;18(10):2101-2113. doi: 10.1021/acschembio.3c00191. Epub 2023 Jun 29.
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Targeting Metalloenzymes: The "Achilles' Heel" of Viruses and Parasites.靶向金属酶：病毒和寄生虫的“阿喀琉斯之踵”
Pharmaceuticals (Basel). 2023 Jun 19;16(6):901. doi: 10.3390/ph16060901.
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Pyrrolyl and Indolyl α-γ-Diketo Acid Derivatives Acting as Selective Inhibitors of Human Carbonic Anhydrases IX and XII.作为人碳酸酐酶IX和XII选择性抑制剂的吡咯基和吲哚基α-γ-二酮酸衍生物
Pharmaceuticals (Basel). 2023 Jan 27;16(2):188. doi: 10.3390/ph16020188.
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Hybrid Molecules as Potential Drugs for the Treatment of HIV: Design and Applications.作为治疗艾滋病潜在药物的杂合分子：设计与应用
Pharmaceuticals (Basel). 2022 Aug 31;15(9):1092. doi: 10.3390/ph15091092.
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Retroviral RNase H: Structure, mechanism, and inhibition.逆转录病毒核糖核酸酶 H：结构、机制与抑制。
Enzymes. 2021;50:227-247. doi: 10.1016/bs.enz.2021.07.007. Epub 2021 Sep 24.
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In Vitro Anti-HIV-1 Reverse Transcriptase and Integrase Properties of L. Leaves, Bark, and Peel Extracts and Their Main Compounds.L. 叶、树皮和果皮提取物及其主要化合物的体外抗HIV-1逆转录酶和整合酶特性
Plants (Basel). 2021 Oct 7;10(10):2124. doi: 10.3390/plants10102124.
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Pyrroles as Privileged Scaffolds in the Search for New Potential HIV Inhibitors.吡咯作为寻找新型潜在HIV抑制剂的优势骨架。
Pharmaceuticals (Basel). 2021 Sep 2;14(9):893. doi: 10.3390/ph14090893.
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HIV-1 Reverse Transcriptase/Integrase Dual Inhibitors: A Review of Recent Advances and Structure-activity Relationship Studies.HIV-1逆转录酶/整合酶双重抑制剂：近期进展及构效关系研究综述
Iran J Pharm Res. 2021 Spring;20(2):333-369. doi: 10.22037/ijpr.2021.115446.15370.
本文引用的文献
1
Identification of highly conserved residues involved in inhibition of HIV-1 RNase H function by Diketo acid derivatives.鉴定参与二酮酸衍生物抑制HIV-1核糖核酸酶H功能的高度保守残基。
Antimicrob Agents Chemother. 2014 Oct;58(10):6101-10. doi: 10.1128/AAC.03605-14. Epub 2014 Aug 4.
2
Basic quinolinonyl diketo acid derivatives as inhibitors of HIV integrase and their activity against RNase H function of reverse transcriptase.作为 HIV 整合酶抑制剂的基本喹喔啉二酮酸衍生物及其对逆转录酶 RNase H 功能的活性。
J Med Chem. 2014 Apr 24;57(8):3223-34. doi: 10.1021/jm5001503. Epub 2014 Apr 11.
3
6-(1-Benzyl-1H-pyrrol-2-yl)-2,4-dioxo-5-hexenoic acids as dual inhibitors of recombinant HIV-1 integrase and ribonuclease H, synthesized by a parallel synthesis approach.6-(1-苄基-1H-吡咯-2-基)-2,4-二氧代-5-己烯酸作为重组 HIV-1 整合酶和核糖核酸酶 H 的双重抑制剂，通过平行合成方法合成。
J Med Chem. 2013 Nov 14;56(21):8588-98. doi: 10.1021/jm401040b. Epub 2013 Nov 5.
4
New anthraquinone derivatives as inhibitors of the HIV-1 reverse transcriptase-associated ribonuclease H function.新型蒽醌衍生物作为 HIV-1 逆转录酶相关核糖核酸酶 H 功能抑制剂。
Chemotherapy. 2012;58(4):299-307. doi: 10.1159/000343101. Epub 2012 Oct 31.
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Activities, crystal structures, and molecular dynamics of dihydro-1H-isoindole derivatives, inhibitors of HIV-1 integrase.二氢-1H-异吲哚衍生物作为 HIV-1 整合酶抑制剂的活性、晶体结构和分子动力学。
ACS Chem Biol. 2013 Jan 18;8(1):209-17. doi: 10.1021/cb300471n. Epub 2012 Dec 24.
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HIV-1 Reverse Transcriptase Still Remains a New Drug Target: Structure, Function, Classical Inhibitors, and New Inhibitors with Innovative Mechanisms of Actions.HIV-1逆转录酶仍然是一个新的药物靶点：结构、功能、经典抑制剂以及具有创新作用机制的新型抑制剂
Mol Biol Int. 2012;2012:586401. doi: 10.1155/2012/586401. Epub 2012 Jun 20.
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Development of a series of 3-hydroxyquinolin-2(1H)-ones as selective inhibitors of HIV-1 reverse transcriptase associated RNase H activity.开发一系列 3-羟基喹啉-2(1H)-酮类化合物作为 HIV-1 逆转录酶相关 RNase H 活性的选择性抑制剂。
Bioorg Med Chem Lett. 2012 Jun 15;22(12):3988-92. doi: 10.1016/j.bmcl.2012.04.096. Epub 2012 Apr 30.
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Identification of HIV-1 reverse transcriptase dual inhibitors by a combined shape-, 2D-fingerprint- and pharmacophore-based virtual screening approach.基于形状、2D 指纹和药效基团的组合虚拟筛选方法鉴定 HIV-1 逆转录酶双重抑制剂。
Eur J Med Chem. 2012 Apr;50:216-29. doi: 10.1016/j.ejmech.2012.01.056. Epub 2012 Feb 5.
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Diketoacid inhibitors of HIV-1 integrase: from L-708,906 to raltegravir and beyond.HIV-1 整合酶的二酮酸抑制剂：从 L-708,906 到拉替拉韦及其他药物。
Curr Med Chem. 2012;19(8):1177-92. doi: 10.2174/092986712799320565.
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Effects of new quinizarin derivatives on both HCV NS5B RNA polymerase and HIV-1 reverse transcriptase associated ribonuclease H activities.新型醌茜衍生物对丙型肝炎病毒NS5B RNA聚合酶和HIV-1逆转录酶相关核糖核酸酶H活性的影响。
J Chemother. 2011 Oct;23(5):273-6. doi: 10.1179/joc.2011.23.5.273.
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