Synthesis and Biological Evaluation of Novel Aryl-2H-pyrazole Derivatives as Potent Non-purine Xanthine Oxidase Inhibitors

被引：11

作者：

Sun, Zhi-Gang ^{[1
]}

Zhou, Xiao-Jing ^{[1
]}

Zhu, Ming-Li ^{[1
]}

Ding, Wen-Ze ^{[1
]}

Li, Zhen ^{[1
]}

Zhu, Hai-Liang ^{[1
]}

机构：

[1] Nanjing Univ, State Key Lab Pharmaceut Biotechnol, Nanjing 210093, Jiangsu, Peoples R China

来源：

CHEMICAL & PHARMACEUTICAL BULLETIN | 2015年 / 63卷 / 08期

关键词：

pyrazole; xanthine oxidase; inhibitory; OXIDOREDUCTASE; DISCOVERY; MECHANISM;

D O I：

10.1248/cpb.c15-00282

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of aryl-2H-pyrazole derivatives were synthesized and evaluated for inhibitory activity against xanthine oxidase in vitro as potent xanthine oxidase inhibitors. Among them, 2 aryl-2H-pyrazole derivatives showed significant inhibitory activities against xanthine oxidase. Compound 19 emerged as the most potent xanthine oxidase inhibitor (IC50=9.8 mu M) in comparison with allopurinol (IC50=9.5 mu M). The docking study revealed that compound 19 might have strong interactions with the active site of xanthine oxidase. This compound is thus a new candidate for further development for the treatment of gout.

引用

页码：603 / 607

页数：5

共 50 条

[41] Effect of febuxostat, a novel non-purine, selective inhibitor of xanthine oxidase (NP-SIXO), on enzymes in purine and pyrimidine metabolism pathway.
Lin, Z
Takano, Y
Horiuchi, H
ARTHRITIS AND RHEUMATISM, 2003, 48 (09): : S531 - S531
[42] Chalcone derivatives as xanthine oxidase inhibitors: synthesis, binding mode investigation, biological evaluation, and ADMET prediction
Yang, Can
Liu, Yi
Tu, Yanbei
Li, Lizi
Du, Jiana
Yu, Dehong
He, Pei
Wang, Tao
Liu, Yan
Chen, Hao
Li, Yanfang
BIOORGANIC CHEMISTRY, 2023, 131
[43] Design, Synthesis, Molecular Modeling and Biological Evaluation of Novel Pyrazole Benzimidazolone Derivatives as Potent Antioxidants
Adardour, Mohamed
Lahcen, Marouane Ait
Oubahmane, Mehdi
Ettahiri, Walid
Hdoufane, Ismail
Bouamama, Hafida
Alanazi, Mohammed M.
Cherqaoui, Driss
Taleb, Mustapha
Garcia, Elena Zaballos
Baouid, Abdesselam
PHARMACEUTICALS, 2023, 16 (12)
[44] Design, synthesis and biological evaluation of novel oseltamivir derivatives as potent neuraminidase inhibitors
Wang, Zhen
Cheng, Li Ping
Zhang, Xing Hua
Pang, Wan
Li, Liang
Zhao, Jin Long
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2017, 27 (24) : 5429 - 5435
[45] Design, Synthesis, and Biological Evaluation of Novel Acylhydrazone Derivatives as Potent Neuraminidase Inhibitors
Li, Meng
Cheng, Li Ping
Pang, Wan
Zhong, Zhi Jian
Guo, Ling Ling
ACS MEDICINAL CHEMISTRY LETTERS, 2020, 11 (09): : 1745 - 1750
[46] Design, synthesis and biological evaluation of novel thiazole derivatives as potent FabH inhibitors
Lv, Peng-Cheng
Wang, Kai-Rui
Yang, Ying
Mao, Wen-Jun
Chen, Jin
Xiong, Jing
Zhu, Hai-Liang
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2009, 19 (23) : 6750 - 6754
[47] Design, synthesis and biological evaluation of novel zanamivir derivatives as potent neuraminidase inhibitors
Cheng, Li Ping
Wang, Tian Chi
Yu, Rao
Li, Meng
Huang, Jin Wen
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, 2018, 28 (23-24) : 3622 - 3629
[48] A phase 2, long term open-label safety and efficacy study of febuxostat, a novel non-purine, selective inhibitor of xanthine oxidase
Schumacher, HE
Wortmann, R
Becke, MA
MacDonald, P
Palo, WA
Eustace, D
Streit, J
Joseph-Ridge, N
ARTHRITIS AND RHEUMATISM, 2004, 50 (09): : S335 - S335
[49] Long-term safety and efficacy of febuxostat, a novel non-purine selective inhibitor of xanthine oxidase, in subjects with hyperuricemia and gout
Schumacher, HR
Wortmann, R
Becker, M
MacDonald, P
Palo, W
Streit, J
Lademacher, C
Joseph-Ridge, N
ANNALS OF THE RHEUMATIC DISEASES, 2005, 64 : 498 - 498
[50] Design, synthesis and biological evaluation of novel xanthine oxidase inhibitors bearing a 2-arylbenzo[b]furan scaffold
Tang, Hong-Jin
Li, Wei
Zhou, Mei
Peng, Li-Ying
Wang, Jin-Xin
Li, Jia-Huang
Chen, Jun
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, 2018, 151 : 849 - 860

← 1 2 3 4 5 →