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Novel HIV-1 non-nucleoside reverse transcriptase inhibitors: a patent review (2011 – 2014)

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Fenju Wei, Dongwei Kang, Srinivasulu Cherukupalli, Waleed A. Zalloum, Tao Zhang, Xinyong Liu & Peng Zhan. (2020) Discovery and optimizing polycyclic pyridone compounds as anti-HBV agents. Expert Opinion on Therapeutic Patents 30:9, pages 715-721.
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Yanjing Wang, Xiangeng Wang, Yi Xiong, Aman Chandra Kaushik, Junaid Muhammad, Abbas Khan, Hao Dai & Dong-Qing Wei. (2020) New strategy for identifying potential natural HIV-1 non-nucleoside reverse transcriptase inhibitors against drug-resistance: an in silico study. Journal of Biomolecular Structure and Dynamics 38:11, pages 3327-3341.
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Xia Hao, Xiaofang Zuo, Dongwei Kang, Jian Zhang, Yuning Song, Xinyong Liu & Peng Zhan. (2019) Contemporary medicinal-chemistry strategies for discovery of blood coagulation factor Xa inhibitors. Expert Opinion on Drug Discovery 14:9, pages 915-931.
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Xiaofang Zuo, Zhipeng Huo, Dongwei Kang, Gaochan Wu, Zhongxia Zhou, Xinyong Liu & Peng Zhan. (2018) Current insights into anti-HIV drug discovery and development: a review of recent patent literature (2014–2017). Expert Opinion on Therapeutic Patents 28:4, pages 299-316.
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Tomasz Frączek, Rafał Kamiński, Agnieszka Krakowiak, Evelien Naessens, Bruno Verhasselt & Piotr Paneth. (2018) Diaryl ethers with carboxymethoxyphenacyl motif as potent HIV-1 reverse transcriptase inhibitors with improved solubility. Journal of Enzyme Inhibition and Medicinal Chemistry 33:1, pages 9-16.
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Dongwei Kang, Zhipeng Huo, Gaochan Wu, Jiabao Xu, Peng Zhan & Xinyong Liu. (2017) Novel fused pyrimidine and isoquinoline derivatives as potent HIV-1 NNRTIs: a patent evaluation of WO2016105532A1, WO2016105534A1 and WO2016105564A1. Expert Opinion on Therapeutic Patents 27:4, pages 383-391.
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Ping Gao, Lin Sun, Junsu Zhou, Xiao Li, Peng Zhan & Xinyong Liu. (2016) Discovery of novel anti-HIV agents via Cu(I)-catalyzed azide-alkyne cycloaddition (CuAAC) click chemistry-based approach. Expert Opinion on Drug Discovery 11:9, pages 857-871.
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Xiao Li, Ping Gao, Peng Zhan & Xinyong Liu. (2016) Substituted indoles as HIV-1 non-nucleoside reverse transcriptase inhibitors: a patent evaluation (WO2015044928). Expert Opinion on Therapeutic Patents 26:5, pages 629-635.
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Boshi Huang, Dongwei Kang, Jiapei Yang, Peng Zhan & Xinyong Liu. (2016) Novel diarylpyrimidines and diaryltriazines as potent HIV-1 NNRTIs with dramatically improved solubility: a patent evaluation of US20140378443A1. Expert Opinion on Therapeutic Patents 26:2, pages 281-289.
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Boshi Huang, Dongwei Kang, Peng Zhan & Xinyong Liu. (2015) Fragment-based approaches to anti-HIV drug discovery: state of the art and future opportunities. Expert Opinion on Drug Discovery 10:12, pages 1271-1281.
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Qing Meng, Na Liu, Boshi Huang, Peng Zhan & Xinyong Liu. (2015) Novel fluorine-containing DAPY derivatives as potent HIV-1 NNRTIs: a patent evaluation of WO2014072419. Expert Opinion on Therapeutic Patents 25:12, pages 1477-1486.
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Articles from other publishers (34)

Jing‐Bo Wang, Meng‐Di Ma, Nan Lu, Yu‐Zhuo Yang, Jin‐Xuan Yang, Yi‐Ming Li, Cong‐Qiang Xie, Ning‐Yu Ma, Rong‐Hua Luo, Yue‐Ping Wang, Liu‐Meng Yang, Hong‐Bin Zhang, Yong‐Tang Zheng & Yan‐Ping He. (2023) Synthesis and anti‐HIV activity of non‐nucleoside reverse‐transcriptase inhibitor DB02 phosphate derivatives based on water‐soluble optimization. Drug Development Research 84:3, pages 465-474.
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Lina Zhang, Fenju Wei, Jiwei Zhang, Chuanfeng Liu, Nerea López-Carrobles, Xinyong Liu, Luis Menéndez-Arias & Peng Zhan. (2022) Current medicinal chemistry strategies in the discovery of novel HIV-1 ribonuclease H inhibitors. European Journal of Medicinal Chemistry 243, pages 114760.
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Zhipeng Fu, Tao Zhang, Zhongxia Zhou, Dongwei Kang, Lin Sun, Shenghua Gao, Srinivasulu Cherukupalli, Erik De Clercq, Christophe Pannecouque, Xinyong Liu & Peng Zhan. (2021) Exploiting the hydrophobic channel of the NNIBP: Discovery of novel diarylpyrimidines as HIV-1 NNRTIs against wild-type and K103N mutant viruses. Bioorganic & Medicinal Chemistry 42, pages 116239.
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Aman Kapoor, Amar Deep Ankalgi, Upasana Thakur, Vinay Pandit & Mahendra Singh Ashawat. (2020) Method Development and Validation for Multicomponent Analysis of Emtricitabine and Ritonavir in Bulk Drug by RP-HPLC. Journal of Drug Delivery and Therapeutics 10:6, pages 137-144.
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Yujie Ren, Yue Ma, Srinivasulu Cherukupalli, John E. Tavis, Luis Menéndez-Arias, Xinyong Liu & Peng Zhan. (2020) Discovery and optimization of benzenesulfonamides-based hepatitis B virus capsid modulators via contemporary medicinal chemistry strategies. European Journal of Medicinal Chemistry 206, pages 112714.
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Eriko Ohsaki & Keiji Ueda. (2020) Screening and Evaluation of Novel Compounds against Hepatitis B Virus Polymerase Using Highly Purified Reverse Transcriptase Domain. Viruses 12:8, pages 840.
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Moaz M. Abdou. (2020) Synopsis of recent synthetic methods and biological applications of phosphinic acid derivatives. Tetrahedron 76:25, pages 131251.
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Pouria Shirvani, Afshin Fassihi, Lotfollah Saghaie, Siska Van Belle, Zeger Debyser & Frauke Christ. (2020) Synthesis, anti-HIV-1 and antiproliferative evaluation of novel 4-nitroimidazole derivatives combined with 5-hydroxy-4-pyridinone moiety. Journal of Molecular Structure 1202, pages 127344.
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Xiangyi Jiang, Ji Yu, Zhongxia Zhou, Jacob Kongsted, Yuning Song, Christophe Pannecouque, Erik De Clercq, Dongwei Kang, Vasanthanathan Poongavanam, Xinyong Liu & Peng Zhan. (2019) Molecular design opportunities presented by solvent‐exposed regions of target proteins. Medicinal Research Reviews 39:6, pages 2194-2238.
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Leandro Battini & Mariela Bollini. (2018) Challenges and approaches in the discovery of human immunodeficiency virus type‐1 non‐nucleoside reverse transcriptase inhibitors. Medicinal Research Reviews 39:4, pages 1235-1273.
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Roberto Romeo, Daniela Iannazzo, Lucia Veltri, Bartolo Gabriele, Beatrice Macchi, Caterina Frezza, Francesca Marino-Merlo & Salvatore V. Giofrè. (2019) Pyrimidine 2,4-Diones in the Design of New HIV RT Inhibitors. Molecules 24:9, pages 1718.
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Stefano Agnello, Michael Brand, Mathieu F. Chellat, Silvia Gazzola & Rainer Riedl. (2019) A Structural View on Medicinal Chemistry Strategies against Drug Resistance. Angewandte Chemie International Edition 58:11, pages 3300-3345.
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Stefano Agnello, Michael Brand, Mathieu F. Chellat, Silvia Gazzola & Rainer Riedl. (2019) Eine strukturelle Evaluierung medizinalchemischer Strategien gegen Wirkstoffresistenzen. Angewandte Chemie 131:11, pages 3336-3383.
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Pouria Shirvani, Afshin Fassihi & Lotfollah Saghaie. (2018) Recent Advances in the Design and Development of Non‐nucleoside Reverse Transcriptase Inhibitor Scaffolds. ChemMedChem 14:1, pages 52-77.
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Giosuè Costa, Roberta Rocca, Angela Corona, Nicole Grandi, Federica Moraca, Isabella Romeo, Carmine Talarico, Maria Giovanna Gagliardi, Francesca Alessandra Ambrosio, Francesco Ortuso, Stefano Alcaro, Simona Distinto, Elias Maccioni, Enzo Tramontano & Anna Artese. (2019) Novel natural non-nucleoside inhibitors of HIV-1 reverse transcriptase identified by shape- and structure-based virtual screening techniques. European Journal of Medicinal Chemistry 161, pages 1-10.
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Boshi Huang, Xinhao Liu, Ye Tian, Dongwei Kang, Zhongxia Zhou, Dirk Daelemans, Erik De Clercq, Christophe Pannecouque, Peng Zhan & Xinyong Liu. (2018) First discovery of a potential carbonate prodrug of NNRTI drug candidate RDEA427 with submicromolar inhibitory activity against HIV-1 K103N/Y181C double mutant strain. Bioorganic & Medicinal Chemistry Letters 28:8, pages 1348-1351.
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Xueyi Lu, Jiapei Yang, Dongwei Kang, Ping Gao, Dirk Daelemans, Erik De Clercq, Christophe Pannecouque, Peng Zhan & Xinyong Liu. (2018) The discovery of novel diarylpyri(mi)dine derivatives with high level activity against a wide variety of HIV-1 strains as well as against HIV-2. Bioorganic & Medicinal Chemistry 26:8, pages 2051-2060.
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KaiJun Jin, Hong Yin, Erik De Clercq, Christophe Pannecouque, Ge Meng & FenEr Chen. (2018) Discovery of biphenyl-substituted diarylpyrimidines as non-nucleoside reverse transcriptase inhibitors with high potency against wild-type and mutant HIV-1. European Journal of Medicinal Chemistry 145, pages 726-734.
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V. T. Valuev-Elliston & S. N. Kochetkov. (2018) Novel HIV-1 non-nucleoside reverse transcriptase inhibitors: A combinatorial approach. Biochemistry (Moscow) 82:13, pages 1716-1743.
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Oscar Méndez-Lucio, J. Jesús Naveja, Hugo Vite-Caritino, Fernando D. Prieto-Martínez & José L. Medina-Franco. 2017. Drug Selectivity. Drug Selectivity 1 29 .
Han Ju, Jian Zhang, Boshi Huang, Dongwei Kang, Bing Huang, Xinyong Liu & Peng Zhan. (2017) Inhibitors of Influenza Virus Polymerase Acidic (PA) Endonuclease: Contemporary Developments and Perspectives. Journal of Medicinal Chemistry 60:9, pages 3533-3551.
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Xiao Li, Ping Gao, Boshi Huang, Zhongxia Zhou, Zhao Yu, Zheng Yuan, Huiqing Liu, Christophe Pannecouque, Dirk Daelemans, Erik De Clercq, Peng Zhan & Xinyong Liu. (2017) Discovery of novel piperidine-substituted indolylarylsulfones as potent HIV NNRTIs via structure-guided scaffold morphing and fragment rearrangement. European Journal of Medicinal Chemistry 126, pages 190-201.
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Dongwei Kang, Heng Zhang, Zhongxia Zhou, Boshi Huang, Lieve Naesens, Peng Zhan & Xinyong Liu. (2016) First discovery of novel 3-hydroxy-quinazoline-2,4(1H,3H)-diones as specific anti-vaccinia and adenovirus agents via ‘privileged scaffold’ refining approach. Bioorganic & Medicinal Chemistry Letters 26:21, pages 5182-5186.
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Petr Šimon, Ondřej Baszczyňski, David Šaman, George Stepan, Eric Hu, Eric B. Lansdon, Petr Jansa & Zlatko Janeba. (2016) Novel (2,6-difluorophenyl)(2-(phenylamino)pyrimidin-4-yl)methanones with restricted conformation as potent non-nucleoside reverse transcriptase inhibitors against HIV-1. European Journal of Medicinal Chemistry 122, pages 185-195.
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Dongwei Kang, Zengjun Fang, Zhenyu Li, Boshi Huang, Heng Zhang, Xueyi Lu, Haoran Xu, Zhongxia Zhou, Xiao Ding, Dirk Daelemans, Erik De Clercq, Christophe Pannecouque, Peng Zhan & Xinyong Liu. (2016) Design, Synthesis, and Evaluation of Thiophene[3,2- d ]pyrimidine Derivatives as HIV-1 Non-nucleoside Reverse Transcriptase Inhibitors with Significantly Improved Drug Resistance Profiles . Journal of Medicinal Chemistry 59:17, pages 7991-8007.
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Xueyi Lu, Xiao Li, Jiapei Yang, Boshi Huang, Dongwei Kang, Fabao Zhao, Zhongxia Zhou, Erik De Clercq, Dirk Daelemans, Christophe Pannecouque, Peng Zhan & Xinyong Liu. (2016) Arylazolyl(azinyl)thioacetanilides. Part 20: Discovery of novel purinylthioacetanilides derivatives as potent HIV-1 NNRTIs via a structure-based bioisosterism approach. Bioorganic & Medicinal Chemistry 24:18, pages 4424-4433.
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Xiao Li, Boshi Huang, Zhongxia Zhou, Ping Gao, Christophe Pannecouque, Dirk Daelemans, Erik De Clercq, Peng Zhan & Xinyong Liu. (2016) Arylazolyl(azinyl)thioacetanilides: Part 19: Discovery of Novel Substituted Imidazo[4,5-b]pyridin-2-ylthioacetanilides as Potent HIV NNRTIs Via a Structure-based Bioisosterism Approach. Chemical Biology & Drug Design 88:2, pages 241-253.
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Kamal K. Sharma, Frédéric Przybilla, Tobias Restle, Julien Godet & Yves Mély. (2016) FRET-based assay to screen inhibitors of HIV-1 reverse transcriptase and nucleocapsid protein. Nucleic Acids Research 44:8, pages e74-e74.
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Peng Zhan, Christophe Pannecouque, Erik De Clercq & Xinyong Liu. (2015) Anti-HIV Drug Discovery and Development: Current Innovations and Future Trends. Journal of Medicinal Chemistry 59:7, pages 2849-2878.
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Hugo Vite-Caritino, Oscar Méndez-Lucio, Héctor Reyes, Alberto Cabrera, Daniel Chávez & José L. Medina-Franco. (2016) Advances in the development of pyridinone derivatives as non-nucleoside reverse transcriptase inhibitors. RSC Advances 6:3, pages 2119-2130.
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Mônica M. Bastos, Carolina C.P. Costa, Talitha C. Bezerra, Fernando de C. da Silva & Núbia Boechat. (2016) Efavirenz a nonnucleoside reverse transcriptase inhibitor of first-generation: Approaches based on its medicinal chemistry. European Journal of Medicinal Chemistry 108, pages 455-465.
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Zengjun Fang, Dongwei Kang, Lingzi Zhang, Boshi Huang, Huiqing Liu, Christophe Pannecouque, Erik De Clercq, Peng Zhan & Xinyong Liu. (2015) Synthesis and Biological Evaluation of a Series of 2-((1-substituted-1 H -1,2,3-triazol-4-yl)methylthio)-6-(naphthalen-1-ylmethyl)pyrimidin-4(3 H )-one As Potential HIV-1 Inhibitors . Chemical Biology & Drug Design 86:4, pages 614-618.
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Dongwei Kang, Zengjun Fang, Boshi Huang, Lingzi Zhang, Huiqing Liu, Christophe Pannecouque, Lieve Naesens, Erik De Clercq, Peng Zhan & Xinyong Liu. (2015) Synthesis and Preliminary Antiviral Activities of Piperidine-substituted Purines against HIV and Influenza A/H1N1 Infections. Chemical Biology & Drug Design 86:4, pages 568-577.
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Boshi Huang, Cuicui Li, Wenmin Chen, Tao Liu, Mingyan Yu, Lu Fu, Yueyue Sun, Huiqing Liu, Erik De Clercq, Christophe Pannecouque, Jan Balzarini, Peng Zhan & Xinyong Liu. (2015) Fused heterocycles bearing bridgehead nitrogen as potent HIV-1 NNRTIs. Part 3: Optimization of [1,2,4]triazolo[1,5-a]pyrimidine core via structure-based and physicochemical property-driven approaches. European Journal of Medicinal Chemistry 92, pages 754-765.
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