Styrylbenzimidazoles. Synthesis and biological activity - part 3.
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.
Vitale
Gabriella
G
Dipartimento Farmaco Chimico Tossicologico, University of Sassari, Via Muroni, 23-07100 Sassari, Italy.
Corona
Paola
P
Loriga
Mario
M
Carta
Antonio
A
Paglietti
Giuseppe
G
Ibba
Cristina
C
Giliberti
Gabriele
G
Loddo
Roberta
R
Marongiu
Esther
E
La Colla
Paolo
P
D000818:Animals; D000998:Antiviral Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D001562:Benzimidazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D002417:Cattle; D002460:Cell Line; D002470:Cell Survival / Q000187:drug effects; D002522:Chlorocebus aethiops; D006224:Cricetinae; D004267:DNA Viruses / Q000187:drug effects*; D004305:Dose-Response Relationship, Drug; D015195:Drug Design; D018067:Flaviviridae / Q000187:drug effects*; D008826:Microbial Sensitivity Tests; D008968:Molecular Conformation; D012328:RNA Viruses / Q000187:drug effects*; D013237:Stereoisomerism; D013329:Structure-Activity Relationship; D013343:Styrenes / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D014709:Vero Cells
D000998:Antiviral Agents; D001562:Benzimidazoles; D013343:Styrenes