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Design, synthesis and biological activity of DB02 amino acid derivatives as HIV-1 non-nucleoside reverse transcriptase inhibitors
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Jin-xuan YANG1, 3, Le YU2, Yu-zhuo YANG2, Rong-hua LUO1, Yan-ping HE2, *, Yong-tang ZHENG1, *
Acta Pharmaceutica Sinica | 2023, 58(2) : 405 - 412
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Acta Pharmaceutica Sinica | 2023, 58(2): 405-412
• Original Articles •
Design, synthesis and biological activity of DB02 amino acid derivatives as HIV-1 non-nucleoside reverse transcriptase inhibitors
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Jin-xuan YANG1, 3, Le YU2, Yu-zhuo YANG2, Rong-hua LUO1, Yan-ping HE2, *, Yong-tang ZHENG1, *
Affiliations
  • 1. Key Laboratory of Animal Models and Human Disease Mechanisms of the Chinese Academy of Sciences, Kunming Institute of Zoology, Chinese Academy of Sciences, Kunming 650223, China
  • 2. Key Laboratory of Medicinal Chemistry for Natural Resource Ministry of Education, School of Chemical Science and Technology, Yunnan University, Kunming 650091, China
  • 3. College of Traditional Chinese Medicine, Yunnan University of Chinese Medicine, Kunming 650500, China
Published: 2023-02-12 doi: 10.16438/j.0513-4870.2022-0739
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To improve the stability of amino acid ester derivatives of DB02, a series of 24 amide derivatives of DB02 amino acids as non-nucleoside HIV-1 reverse transcriptase inhibitor were designed and synthesized based on bioisosterism by replacing amino acid ester scaffold with more stable amide bond. The anti-HIV-1 activity of these compounds was evaluated by MTT assay and counting the number of syncytia. Most of the target compounds showed a potential anti-HIV-1 activity, among which compounds 2d, 2i, 2l, 2s, and 2w had better antiviral effect than lead compound DB02, with a therapeutic index > 1 000.00. Finally, the structure-activity relationship of these compounds was discussed, which provided new ideas for the further development of DB02 derivatives.

DB02  /  non-nucleoside reverse transcriptase inhibitor  /  amino acid amide derivative  /  anti-HIV-1 activity  /  structure-activity relationship
Jin-xuan YANG, Le YU, Yu-zhuo YANG, Rong-hua LUO, Yan-ping HE, Yong-tang ZHENG. Design, synthesis and biological activity of DB02 amino acid derivatives as HIV-1 non-nucleoside reverse transcriptase inhibitors[J]. Acta Pharmaceutica Sinica, 2023 , 58 (2) : 405 -412 . DOI: 10.16438/j.0513-4870.2022-0739
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doi: 10.16438/j.0513-4870.2022-0739
  • Receive Date：2022-06-16
  • Online Date：2025-11-21
  • Published：2023-02-12
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History
  • Received：2022-06-16
  • Revised：2022-07-18
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Affiliations
    1. Key Laboratory of Animal Models and Human Disease Mechanisms of the Chinese Academy of Sciences, Kunming Institute of Zoology, Chinese Academy of Sciences, Kunming 650223, China
    2. Key Laboratory of Medicinal Chemistry for Natural Resource Ministry of Education, School of Chemical Science and Technology, Yunnan University, Kunming 650091, China
    3. College of Traditional Chinese Medicine, Yunnan University of Chinese Medicine, Kunming 650500, China
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表12种不同金属材料的力学参数
科
Family		 属数
Number of
genus		 种数
Number of
species		 占总种数比例
Percentage of
total species (%)		 属
Genus		 种数
Number of
species		 占总种数比例
Percentage of total
species (%)
鹅膏菌科Amanitaceae 2 11 5.26 鹅膏菌属 Amanita 10 4.78
小菇科 Mycenaceae 2 12 5.74 丝盖伞属 Inocybe 5 2.39
多孔菌科 Polyporaceae 8 14 6.70 蜡蘑属 Laccaria 5 2.39
红菇科 Russulaceae 3 23 11.00 小皮伞属 Marasmius 6 2.87
小菇属 Mycena 11 5.26
光柄菇属 Pluteus 5 2.39
红菇属 Russula 17 8.13
栓菌属 Trametes 5 2.39
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