Synthesis and pharmacological evaluation of choroquine derivatives bearing long aminated side chains as antivirus and anti-inflammatory agents

doi:10.1016/j.bioorg.2021.105346

	Synthesis and pharmacological evaluation of choroquine derivatives bearing long aminated side chains as antivirus and anti-inflammatory agents
	Song, Zilan 1,2,3,4; Liu, Yuting 2,4; Xie, Chenghu 3; Tong, Xiankun 2,4; Wang, Xue 2,4; Zhou, Yu 2,4; Gu, Wangting 3; Zuo, Jianping 2,4; He, Shijun 2,4; Zhang, Ao 1,2,3,4,5
刊名	BIOORGANIC CHEMISTRY
	2021-11-01
卷号	116 页码:8
关键词	Choroquine Aminochloroquine Antivirus Anti-inflammatory Cytokines
ISSN号	0045-2068
DOI	10.1016/j.bioorg.2021.105346
通讯作者	Zuo, Jianping(jpzuo@simm.ac.cn) ; He, Shijun(heshijun@simm.ac.cn) ; Zhang, Ao(ao6919zhang@sjtu.edu.cn)
英文摘要	Starting from the antimalarial drugs chloroquine and hydroxychloroquine, we conducted a structural optimization on the side chain of chloroquine by introducing amino substituted longer chains thus leading to a series of novel aminochloroquine derivatives. Anti-infectious effects against SARS-Cov2 spike glycoprotein as well as immunosuppressive and anti-inflammatory activities of the new compounds were evaluated. Distinguished immunosuppressive activities on the responses of T cell, B cell and macrophages upon mitogen and pathogenic signaling were manifested. Compounds 9-11 displayed the most promising inhibitory effects both on cellular proliferation and on the production of multiple pro-inflammatory cytokines, including IL-17, IFN-gamma, IL-6, IL-1 beta and TNF-alpha, which might be insightful in the pursuit of treatment for immune disorders and inflammatory diseases.
资助项目	National Natural Science Foundation of China[82173653] ; National Natural Science Foundation of China[81773565] ; National Natural Science Foundation of China[81871240] ; Shanghai Municipal Science and Technology Major Project[TM202101L004] ; Biomedical Technology Innovation Project[21S11907700] ; Biomedical Technology Innovation Project[21S11911000] ; Shanghai Jiao Tong University[AF1700037] ; Shanghai Jiao Tong University[WF220217002] ; Shanghai Jiao Tong University[WH101117001]
WOS研究方向	Biochemistry & Molecular Biology ; Chemistry
语种	英语
出版者	ACADEMIC PRESS INC ELSEVIER SCIENCE
WOS记录号	WOS:000702879500002
内容类型	期刊论文
源URL	[http://119.78.100.183/handle/2S10ELR8/297567]
专题	中国科学院上海药物研究所
通讯作者	Zuo, Jianping; He, Shijun; Zhang, Ao
作者单位	1.Nanjing Univ Chinese Med, Sch Chinese Mat Med, Nanjing 210023, Peoples R China 2.Chinese Acad Sci, Shanghai Inst Mat Med SIMM, State Key Lab Drug Res, Shanghai 201203, Peoples R China 3.Shanghai Jiao Tong Univ, Pharm X Ctr, Sch Pharmaceut Sci, Shanghai 200240, Peoples R China 4.Univ Chinese Acad Sci, Beijing 100049, Peoples R China 5.ShanghaiTech Univ, Sch Life Sci & Technol, Shanghai 201210, Peoples R China
推荐引用方式 GB/T 7714	Song, Zilan,Liu, Yuting,Xie, Chenghu,et al. Synthesis and pharmacological evaluation of choroquine derivatives bearing long aminated side chains as antivirus and anti-inflammatory agents[J]. BIOORGANIC CHEMISTRY,2021,116:8.
APA	Song, Zilan.,Liu, Yuting.,Xie, Chenghu.,Tong, Xiankun.,Wang, Xue.,...&Zhang, Ao.(2021).Synthesis and pharmacological evaluation of choroquine derivatives bearing long aminated side chains as antivirus and anti-inflammatory agents.BIOORGANIC CHEMISTRY,116,8.
MLA	Song, Zilan,et al."Synthesis and pharmacological evaluation of choroquine derivatives bearing long aminated side chains as antivirus and anti-inflammatory agents".BIOORGANIC CHEMISTRY 116(2021):8.