Synthesis and pharmacological evaluation of choroquine derivatives bearing long aminated side chains as antivirus and anti-inflammatory agents.
Bioorg Chem
; 116: 105346, 2021 11.
Article
in English
| MEDLINE | ID: covidwho-1401246
ABSTRACT
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-1ß and TNF-α, which might be insightful in the pursuit of treatment for immune disorders and inflammatory diseases.
Keywords
Full text:
Available
Collection:
International databases
Database:
MEDLINE
Main subject:
Antiviral Agents
/
Chloroquine
/
Anti-Inflammatory Agents, Non-Steroidal
/
Spike Glycoprotein, Coronavirus
/
Amines
/
SARS-CoV-2
Type of study:
Experimental Studies
Limits:
Humans
Language:
English
Journal:
Bioorg Chem
Year:
2021
Document Type:
Article
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