Bis(benzofuran-thiazolidinone)s and bis(benzofuran-thiazinanone)s as inhibiting agents for chikungunya virus.
There are currently still no approved antiviral drugs to treat or prevent chikungunya virus (CHIKV) infections despite the fact that this arbovirus continues to cause outbreaks in Africa, Asia, and South- and Central-America. Thus 20 new conjugated compounds in the families of bis(benzofuran-1,3-thiazolidin-4-one)s and bis(benzofuran-1,3-thiazinan-4-one)s were designed based on the structural features of suramin. These new compounds were synthesized by chemical methods and their structures were confirmed spectroscopically. In CPE reduction assays, six of these new bis-conjugates inhibited CHIKV replication in Vero E6 cells with EC50 in the range of 1.9-2.7 μM and selectivity index values of ∼75 or higher. These results and compounds provide a starting point for further optimization, design, and synthesis of new antiviral agents for this (re)emerging disease.
['Hwu|Jih Ru|JR|', 'Gupta|Nitesh K|NK|', 'Tsay|Shwu-Chen|SC|', 'Huang|Wen-Chieh|WC|', 'Albulescu|Irina C|IC|', 'Kovacikova|Kristina|K|', 'van Hemert|Martijn J|MJ|']
D000818:Animals D000998:Antiviral Agents D001572:Benzofurans D002460:Cell Line D065632:Chikungunya Fever D002646:Chikungunya virus D002522:Chlorocebus aethiops D015195:Drug Design D006801:Humans D013498:Suramin D013843:Thiazines D014709:Vero Cells D014779:Virus Replication
Chikungunya virus Antiviral Suramin Benzofuran Thiazinanone Thiazolidinone