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Design, synthesis and biological evaluation of amide derivatives as xanthine oxidase inhibitors
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Lei ZHANG1, Ding-an YAN1, Jin-ying TIAN2, Fei YE2, Zhi-yan XIAO1, *
Acta Pharmaceutica Sinica | 2017, 52(6) : 952 - 958
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Acta Pharmaceutica Sinica | 2017, 52(6): 952-958
• ORIGINAL ARTICLES·Medicinal Chemistry •
Design, synthesis and biological evaluation of amide derivatives as xanthine oxidase inhibitors
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Lei ZHANG1, Ding-an YAN1, Jin-ying TIAN2, Fei YE2, Zhi-yan XIAO1, *
Affiliations
  • 1. Beijing Key Laboratory of Active Substance Discovery and Druggability Evaluation, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China
  • 2. 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: 2017-06-12 doi: 10.16438/j.0513-4870.2017-0251
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Xanthine oxidase (XO) is a key enzyme in the synthesis of uric acid. Therefore, XO inhibitors play an important role in the antihyperuricemic therapy. Based on the template structures of febuxostat and topiroxostat, 18 amide derivatives were designed and synthesized. Among them, six showed apparent inhibitory activity against XO under the concentration of 10 μmol·L-1. Molecular docking revealed the possible interaction mode of this compound class, which may provide a clue for further molecular design.

xanthine oxidase  /  hyperuricemia  /  gout  /  amide derivative
Lei ZHANG, Ding-an YAN, Jin-ying TIAN, Fei YE, Zhi-yan XIAO. Design, synthesis and biological evaluation of amide derivatives as xanthine oxidase inhibitors[J]. Acta Pharmaceutica Sinica, 2017 , 52 (6) : 952 -958 . DOI: 10.16438/j.0513-4870.2017-0251
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Article Info
doi: 10.16438/j.0513-4870.2017-0251
  • Receive Date：2017-03-22
  • Online Date：2026-01-14
  • Published：2017-06-12
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History
  • Received：2017-03-22
  • Revised：2017-04-11
Funding
Affiliations
    1. Beijing Key Laboratory of Active Substance Discovery and Druggability Evaluation, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China
    2. 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
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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