Work

Synthesis and evaluation of the activity of 1H-1,2,3-triazole-thiophene ester derivatives against Chikungunya virus

Year: 2024

Type: article

Abstract: The Chikungunya virus (CHIKV), transmitted by mosquitoes, recently caused severe outbreaks from the Indian Ocean to the Americas. Despite prior research on alphaviruses , little was understood about CHIKV's biology during the 2005 epidemic. This study tested 16 esters of 1H-1,2,3-triazole-thiophene to assess their cytotoxicity and antiviral activity . Six substances (11d, 11 f, 11 h, 12c, 12d, and 12 f) showed low cytotoxicity and high potential in inhibiting CHIKV in both Vero cells and MG-63 osteoblasts. Effective concentrations (EC50) varied between 0.95 for substance 12 f and 1.5 for substance 11 f, indicating strong inhibitory effects. Compounds 11 f and 12c had virucidal effects, inhibiting approximately 70 % and 55 % of the virus, respectively. Substance 12 f displayed potent inhibition even 12 hours post-infection. Combining 12 f with Ribavirin showed a strong synergistic effect, enhancing antiviral activity. These compounds present potential as selective and effective agents against CHIKV, especially given their post-infection administration capability, potentially paving the way for novel drugs to combat CHIKV outbreaks.

Source: The Microbe

DOI: 10.1016/j.microb.2024.100220