Article ; Online: Design, synthesis, and biological evaluation of N-arylpiperazine derivatives as interferon inducers.
Bioorganic & medicinal chemistry letters
2020 Volume 30, Issue 24, Page(s) 127613
Abstract: ... structure-activity relationship, we designed and synthesized a series of ARP analogues and evaluated the ability to stimulate IFN ... In this study, we assessed arylpiperazine (ARP) as a new core skeleton of IFN inducer. To investigate ... Type I Interferon (IFN) signaling plays an important role in the immune defense system against ...
| Abstract | Type I Interferon (IFN) signaling plays an important role in the immune defense system against virus infection and in the innate immune response, thus IFNs are widely used as anti-viral agents and treatment for immune disorder or cancer. However, there is a growing demand for novel small-molecule IFN inducer due to tolerance, toxicity, or short duration of action following direct administration of IFNs. In this study, we assessed arylpiperazine (ARP) as a new core skeleton of IFN inducer. To investigate structure-activity relationship, we designed and synthesized a series of ARP analogues and evaluated the ability to stimulate IFN response in THP-1 human monocyte cells. Compound 5i was identified as a potent type I IFN inducer as it significantly increased cytokine secretion and increased expression of various IFN-stimulating genes which are representative biomarkers of type I IFN pathway. Our results suggested a beneficial therapeutic potential of 5i as an anti-viral agent. |
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| MeSH term(s) | Drug Design ; Humans ; Immunity, Innate/drug effects ; Interferon Inducers/chemical synthesis ; Interferon Inducers/chemistry ; Interferon Inducers/pharmacology ; Interferon Type I/agonists ; Interferon Type I/immunology ; Monocytes/drug effects ; Monocytes/immunology ; Piperazines/chemical synthesis ; Piperazines/chemistry ; Piperazines/pharmacology ; THP-1 Cells | |||||
| Chemical Substances | Interferon Inducers ; Interferon Type I ; Piperazines | |||||
| Keywords | covid19 | |||||
| Language | English | |||||
| Publishing date | 2020-10-16 | |||||
| Publishing country | England | |||||
| Document type | Journal Article ; Research Support, Non-U.S. Gov't | |||||
| ZDB-ID | 1063195-1 | |||||
| ISSN | 1464-3405 ; 0960-894X | |||||
| ISSN (online) | 1464-3405 | |||||
| ISSN | 0960-894X | |||||
| DOI | 10.1016/j.bmcl.2020.127613 | |||||
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| Database | MEDical Literature Analysis and Retrieval System OnLINE |
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