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Design, synthesis and evaluation of oxadiazoles as novel XO inhibitors
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Hong-zhan WANG1, 2, Ya-jun YANG2, Ying YANG2, Fei YE3, Jin-ying TIAN3, Chuan-ming ZHANG1, *, Zhi-yan XIAO2
Acta Pharmaceutica Sinica | 2025, 60(1) : 164 - 171
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Acta Pharmaceutica Sinica | 2025, 60(1): 164-171
• Original Articles •
Design, synthesis and evaluation of oxadiazoles as novel XO inhibitors
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Hong-zhan WANG1, 2, Ya-jun YANG2, Ying YANG2, Fei YE3, Jin-ying TIAN3, Chuan-ming ZHANG1, *, Zhi-yan XIAO2
Affiliations
  • 1. School of Pharmacy, Baotou Medical College, Inner Mongolia University of Science and Technology, Baotou 014040
  • 2. Beijing Key Laboratory of Active Substance Discovery and Druggability Evaluation, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China
  • 3. Beijing Key Laboratory of New Drug Mechanisms and Pharmacological Evaluation Study, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China
Published: 2025-01-12 doi: 10.16438/j.0513-4870.2024-0820
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Xanthine oxidase (XO) is an important therapeutic target for the treatment of hyperuricemia and gout. Based on the previously identified potent XO inhibitor 1, seventeen oxadiazoles and their ring-opening analogues were designed and synthesized via the bioisostere replacement strategy. Among them, compounds 2l, 2n, and 3b showed obvious XO inhibitory activity at the concentration of 10 μmol·L-1, and compound 3b exhibited an IC50 value of 1.45 μmol·L-1.

xanthine oxidase  /  xanthine oxidase inhibitor  /  oxadiazole  /  hyperuricemia  /  gout
Hong-zhan WANG, Ya-jun YANG, Ying YANG, Fei YE, Jin-ying TIAN, Chuan-ming ZHANG, Zhi-yan XIAO. Design, synthesis and evaluation of oxadiazoles as novel XO inhibitors[J]. Acta Pharmaceutica Sinica, 2025 , 60 (1) : 164 -171 . DOI: 10.16438/j.0513-4870.2024-0820
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Year 2025 volume 60 Issue 1
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Article Info
doi: 10.16438/j.0513-4870.2024-0820
  • Receive Date：2024-08-26
  • Online Date：2025-11-07
  • Published：2025-01-12
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History
  • Received：2024-08-26
  • Revised：2024-11-04
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Affiliations
    1. School of Pharmacy, Baotou Medical College, Inner Mongolia University of Science and Technology, Baotou 014040
    2. Beijing Key Laboratory of Active Substance Discovery and Druggability Evaluation, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China
    3. Beijing Key Laboratory of New Drug Mechanisms and Pharmacological Evaluation Study, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, 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
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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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