Synthesis and pharmacological evaluation of choroquine derivatives bearing long aminated side chains as antivirus and anti-inflammatory agents.
Synthesis and pharmacological evaluation of choroquine derivatives bearing long aminated side chains as antivirus and anti-inflammatory agents.
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具有长胺化侧链的氯喹衍生物的合成及抗病毒抗炎药的药理评价
DOI：
10.1016/j.bioorg.2021.105346
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发表时间：
2021-11
影响因子：
5.1
通讯作者：
Zhang A
中科院分区：
文献类型：
--
作者：
Song Z;Liu Y;Xie C;Tong X;Wang X;Zhou Y;Gu W;Zuo J;He S;Zhang A
我们从抗疟疾药物氯喹和羟氯喹出发，通过引入氨基取代的较长链对氯喹的侧链进行结构优化，合成了一系列新型的氨基氯喹衍生物。评价了新化合物对SARS-Cov2刺激性糖蛋白的抗感染作用以及免疫抑制和抗炎活性。在T细胞、B细胞和巨噬细胞对有丝分裂原和致病信号的反应中表现出明显的免疫抑制活性。化合物9-11显示出最有希望的抑制细胞增殖和多种促炎细胞因子的产生的作用，包括IL-17、干扰素-γ、IL-6、IL-1β和肿瘤坏死因子-α，这可能对免疫紊乱和炎症性疾病的治疗有一定的指导意义。
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-γ, IL-6, IL-1β and TNF-α, which might be insightful in the pursuit of treatment for immune disorders and inflammatory diseases.
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DOI：
10.1016/j.rdc.2016.03.010
发表时间：
2016-08
期刊：
Rheumatic diseases clinics of North America
影响因子：
--
作者：
Vivino FB;Carsons SE;Foulks G;Daniels TE;Parke A;Brennan MT;Forstot SL;Scofield RH;Hammitt KM
通讯作者：
Hammitt KM
影响因子：
158.5
作者：
Boulware, David R.;Pullen, Matthew F.;Hullsiek, Kathy H.
通讯作者：
Hullsiek, Kathy H.
影响因子：
11.8
作者：
Yao, Xueting;Ye, Fei;Liu, Dongyang
通讯作者：
Liu, Dongyang
影响因子：
3.7
作者：
Laplana M;Yuguero O;Fibla J
通讯作者：
Fibla J
影响因子：
5.6
作者：
Hou, Li-Fei;He, Shi-Jun;Zuo, Jian-Ping
通讯作者：
Zuo, Jian-Ping