| Autor: |
Jih Ru Hwu, Avijit Panja, Srinivasan Jayakumar, Shwu-Chen Tsay, Kui-Thong Tan, Wen-Chieh Huang, Yu-Chen Hu, Pieter Leyssen, Johan Neyts |
| Jazyk: |
angličtina |
| Rok vydání: |
2020 |
| Předmět: |
|
| Zdroj: |
Molecules, Vol 25, Iss 17, p 3821 (2020) |
| Druh dokumentu: |
article |
| ISSN: |
1420-3049 |
| DOI: |
10.3390/molecules25173821 |
| Popis: |
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 EC50 = 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 EC50 = 2.29 μM. |
| Databáze: |
Directory of Open Access Journals |
| Externí odkaz: |
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