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Development of Novel N-hydroxypyridone Derivatives as Potential Anti-Ischemic Stroke Agents

文献类型：期刊论文

作者Hu, Linghao1,2; Feng, Hongxuan3,4; Zhang, Hongguang3; Yu, Songda5; Zhao, Qinyuan3,4; Wang, Wei3; Bao, Fengxia3; Ding, Xun3,4; Hu, Jiajing2; Wang, Manjiong1,2
刊名JOURNAL OF MEDICINAL CHEMISTRY
出版日期2020-02-13
卷号63期号:3页码:1051-1067
ISSN号0022-2623
DOI10.1021/acs.jmedchem.9b01338
通讯作者Mao, Fei(maofei@ecust.edu.cn) ; Zhang, Haiyan(hzhang@simm.ac.cn) ; Li, Jian(jianli@ecust.edu.cn)
英文摘要Our previous study had identified ciclopirox (CPX) as a promising lead compound for treatment of ischemic stroke. To find better neuroprotective agents, a series of N-hydroxypyridone derivatives based on CPX were designed, synthesized, and evaluated in this study. Among these derivatives, compound 11 exhibits significant neuroprotection against oxygen glucose deprivation and oxidative stress -induced injuries in neuronal cells. Moreover, compound 11 possesses good blood-brain barrier permeability and superior antioxidant capability. In addition, a complex of compound 11 with olamine-11.01a possesses good water solubility, negligible hERG inhibition, and superior metabolic stability. The in vivo experiment demonstrates that 11.01a significantly reduces brain infarction and alleviates neurological deficits in middle cerebral artery occlusion rats. Hence, compound 11.01a is identified in our research as a prospective prototype in the innovation of stroke treatment.
WOS关键词MECHANISMS ; ANTIOXIDANT ; INHIBITION ; DISCOVERY ; ISCHEMIA ; NXY-059
资助项目National Natural Science Foundation of China[81872747] ; National Natural Science Foundation of China[21672064] ; National Natural Science Foundation of China[81872859] ; National Natural Science Foundation of China[81661148046] ; National Key R&D Program of China[2017YFB0202600] ; Innovative Research Team of High-level Local Universities in Shanghai ; National Special Fund for State Key Laboratory of Bioreactor Engineering[2060204] ; Shanghai Sailing Program[17YF1403600]
WOS研究方向Pharmacology & Pharmacy
语种英语
出版者AMER CHEMICAL SOC
WOS记录号WOS:000514221700011
源URL[http://119.78.100.183/handle/2S10ELR8/281352]  
专题中国科学院上海药物研究所
通讯作者Mao, Fei; Zhang, Haiyan; Li, Jian
作者单位1.East China Univ Sci & Technol, Sch Pharm, State Key Lab Bioreactor Engn, Shanghai 200237, Peoples R China
2.East China Univ Sci & Technol, Sch Pharm, Shanghai Key Lab New Drug Design, Shanghai 200237, Peoples R China
3.Chinese Acad Sci, Shanghai Inst Mat Med, CAS Key Lab Receptor Res, Shanghai 201203, Peoples R China
4.Univ Chinese Acad Sci, Beijing 100049, Peoples R China
5.Chinese Acad Sci, Shanghai Inst Mat Med, Shanghai 201203, Peoples R China
推荐引用方式
GB/T 7714		 Hu, Linghao,Feng, Hongxuan,Zhang, Hongguang,et al. Development of Novel N-hydroxypyridone Derivatives as Potential Anti-Ischemic Stroke Agents[J]. JOURNAL OF MEDICINAL CHEMISTRY,2020,63(3):1051-1067.
APA Hu, Linghao.,Feng, Hongxuan.,Zhang, Hongguang.,Yu, Songda.,Zhao, Qinyuan.,...&Li, Jian.(2020).Development of Novel N-hydroxypyridone Derivatives as Potential Anti-Ischemic Stroke Agents.JOURNAL OF MEDICINAL CHEMISTRY,63(3),1051-1067.
MLA Hu, Linghao,et al."Development of Novel N-hydroxypyridone Derivatives as Potential Anti-Ischemic Stroke Agents".JOURNAL OF MEDICINAL CHEMISTRY 63.3(2020):1051-1067.

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来源：上海药物研究所

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