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Styrylbenzimidazoles. Synthesis and Biological Activity - Part 3

[ Vol. 6 , Issue. 2 ]

Author(s):

Gabriella Vitale, Paola Corona, Mario Loriga, Antonio Carta, Giuseppe Paglietti, Cristina Ibba, Gabriele Giliberti, Roberta Loddo, Esther Marongiu and Paolo La Colla   Pages 70 - 78 ( 9 )

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 μM; among them, compound 17 was the most active, with an EC50 = 1.7 μM. Compounds 18 and 21 were equally active against CVB-2, with EC50 values of 7 — 8 μM, while the derivative 30 was active against RSV with EC50= 1 μM and represents a new lead compound.

Keywords:

Antiviral activity, flaviridae, benzimidazoles

Affiliation:

Dipartimento Farmaco Chimico Tossicologico, University of Sassari, Via Muroni,23-07100 Sassari, Italy.



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