Discovery of lipoic acid-4-phenyl-1H-pyrazole hybrids as novel bifunctional ROCK inhibitors with antioxidant activity

被引：6

作者：

Tu, Ya-lin ^{[1
,2
,3
]}

Chen, Qiu-he ^{[1
,2
,3
]}

Wang, Sheng-nan ^{[1
,2
,3
]}

Uri, Asko ^{[4
]}

Yang, Xiao-hong ^{[1
,2
,3
]}

Chu, Jia-qi ^{[1
,2
,3
]}

Chen, Jing-kao ^{[1
,2
,3
]}

Luo, Bing-ling ^{[2
,5
]}

Chen, Xiao-hong ^{[6
]}

Wen, Shi-jun ^{[2
,5
]}

Pi, Rong-biao ^{[1
,2
,3
,7
]}

机构：

[1] Sun Yat Sen Univ, Sch Pharmaceut Sci, Guangzhou 510006, Guangdong, Peoples R China

[2] Int Joint Lab SYSU PolyU HK Novel Antidemenita Dr, Guangzhou 510006, Guangdong, Peoples R China

[3] Sun Yat Sen Univ, Nat & Local United Engn Lab Druggabil & New Drugs, Guangzhou, Guangdong, Peoples R China

[4] Univ Tartu, Inst Chem, Ravila St, EE-50411 Tartu, Estonia

[5] Sun Yat Sen Univ, Collaborat Innovat Ctr Canc Med, State Key Lab Oncol South China, Ctr Canc, 651 Dongfeng East Rd, Guangzhou 510060, Guangdong, Peoples R China

[6] Sun Yat Sen Univ, Dept Neurol, Affiliated Hosp 3, Guangzhou 510275, Guangdong, Peoples R China

[7] Sun Yat Sen Univ, Zhongshan Sch Med, Guangdong Prov Key Lab Brain Funct & Dis, Guangzhou 510080, Guangdong, Peoples R China

来源：

RSC ADVANCES | 2016年 / 6卷 / 63期

关键词：

RHO KINASE INHIBITORS; NERVOUS-SYSTEM DISORDERS; ALZHEIMERS-DISEASE; NEUROLOGICAL DISORDERS; OXIDATIVE STRESS; POTENT; ACID; FASUDIL; DESIGN; MODEL;

D O I：

10.1039/c6ra12081d

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

A series of lipoic acid (LA) and 4-phenyl-1H-pyrazole hybrids as bifunctional Rho-associated kinase (ROCK) inhibitors were designed, synthesized and evaluated. Compound 15 is identified to be a novel potent bifunctional ROCK inhibitor with antioxidant activity and neuroprotection.

引用

页码：58516 / 58520

页数：5

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