Enterovirus Inhibition by Hinged Aromatic Compounds with Polynuclei

The modern world has no available drugs for the treatment of enteroviruses (EV), which affect millions of people worldwide each year. The EV71 is a major causative disease for hand, foot, and mouth disease; sometimes it is associated with severe central nervous system diseases. Treatment for enterov...

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Bibliographic Details
Published in:Molecules (Basel, Switzerland) Switzerland), 2020-08, Vol.25 (17), p.3821
Main Authors: Hwu, Jih Ru, Panja, Avijit, Jayakumar, Srinivasan, Tsay, Shwu-Chen, Tan, Kui-Thong, Huang, Wen-Chieh, Hu, Yu-Chen, Leyssen, Pieter, Neyts, Johan
Format: Article
Language:English
Subjects:
Animals
Antiviral activity
Antiviral agents
Antiviral Agents - chemical synthesis
Antiviral Agents - chemistry
Antiviral Agents - pharmacology
Aromatic compounds
Aseptic meningitis
Benzene
Carbon
Central nervous system
Central nervous system diseases
Chemical synthesis
Chlorocebus aethiops
Disease
Drugs
enterovirus
Enterovirus A, Human - growth & development
Enterovirus Infections - drug therapy
Enterovirus Infections - metabolism
Enteroviruses
furan
Hand-foot-and-mouth disease
Health services
hinged bond
Hydrocarbons
Infections
Medical treatment
Meningitis
Morpholine
Pyrazole
RNA polymerase
Selectivity
thiophene
Vero Cells
Viruses
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Summary:The modern world has no available drugs for the treatment of enteroviruses (EV), which affect millions of people worldwide each year. The EV71 is a major causative disease for hand, foot, and mouth disease; sometimes it is associated with severe central nervous system diseases. Treatment for enteroviral infection is mainly supportive; treatment for aseptic meningitis caused by enteroviruses is also generally symptomatic. Upon the urgent request of new anti-enterovirus drugs, a series of hinged aromatic compounds with polynulei were synthesized through two different chemical pathways. Among these morpholine-furan/thiophene/pyrrole-benzene-pyrazole conjugates, three new agents exhibited inhibitory activity with EC = 2.29-6.16 μM toward EV71 strain BrCr in RD cells. Their selectivity index values were reached as high as 33.4. Their structure-activity relationship was deduced that a thiophene derivative with morpholine and trifluorobenzene rings showed the greatest antiviral activity, with EC = 2.29 μM.
ISSN:1420-3049
1420-3049
DOI:10.3390/molecules25173821