1. Styrylbenzimidazoles. Synthesis and biological activity - part 3
- Author
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Roberta Loddo, Gabriele Giliberti, Cristina Ibba, Mario Loriga, Paola Corona, Antonio Carta, Giuseppe Paglietti, Paolo La Colla, Gabriella Vitale, and Esther Marongiu
- Subjects
Paramyxoviridae ,Cell Survival ,viruses ,Picornaviridae ,Molecular Conformation ,Reoviridae ,Microbial Sensitivity Tests ,Antiviral Agents ,Cell Line ,Styrenes ,Flaviviridae ,Structure-Activity Relationship ,Cricetinae ,Drug Discovery ,Chlorocebus aethiops ,Animals ,RNA Viruses ,Poxviridae ,Vero Cells ,biology ,Dose-Response Relationship, Drug ,DNA Viruses ,DNA virus ,RNA virus ,Stereoisomerism ,Rhabdoviridae ,biology.organism_classification ,Virology ,Drug Design ,Benzimidazoles ,Cattle - Abstract
As a follow up of an anti-Flaviviridae project, a new series of variously substituted 2-styryl-benzimidazoles were synthesized and tested in vitro for biological activity. Compounds were tested in cell-based assays against viruses representative of: i) two of the three genera of the Flaviviridae family, i.e. Pestiviruses and Flaviviruses; ii) other RNA virus families, such as Retroviridae, Picornaviridae, Paramyxoviridae, Rhabdoviridae and Reoviridae; iii) two DNA virus families (Herpesviridae and Poxviridae) as well as for cytotoxicity tests, run in parallel with antiviral assays,against MDBK, BHK and Vero 76 cells. In the series examined, new leads emerged against BVDV, CVB-2 and RSV. Compounds 11, 12, 17, 18, 24, 31 exhibited anti-BVDV activity in the concentration range 1.7-16 microM; among them, compound 17 was the most active, with an EC(50) = 1.7 microM. Compounds 18 and 21 were equally active against CVB-2, with EC(50) values of 7 - 8 microM, while the derivative 30 was active against RSV with EC(50)= 1 microM and represents a new lead compound.
- Published
- 2010