Antiviral Activity of Benzimidazole Derivatives. I. Antiviral Activity of 1-Substituted-2-[(Benzotriazol-1/2-yl)methyl]benzimidazoles

Forty‐three 2‐[(benzotriazol‐1/2‐yl)methyl]benzimidazoles, bearing either linear (dialkylamino)alkyl‐ or bulkier (quinolizidin‐1‐yl)alkyl moieties at position 1, were evaluated in cell‐based assays for cytotoxicity and antiviral activity against viruses representative of two of the three genera of t...

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Published in:Chemistry & biodiversity 2008-11, Vol.5 (11), p.2386-2401
Main Authors: Tonelli, Michele, Paglietti, Giuseppe, Boido, Vito, Sparatore, Fabio, Marongiu, Fabio, Marongiu, Esther, La Colla, Paolo, Loddo, Roberta
Format: Article
Language:English
Subjects:
Animals
Antiviral activity
Antiviral Agents - chemistry
Antiviral Agents - pharmacology
Antiviral Agents - toxicity
Benzimidazole derivatives
Benzimidazoles - chemistry
Benzimidazoles - pharmacology
Benzimidazoles - toxicity
Benzotriazole derivatives
Cells, Cultured
DNA Viruses - drug effects
Drug Evaluation, Preclinical
Flavivirus - drug effects
Haplorhini
Humans
Pestivirus - drug effects
Quinolizidine derivatives
Respiratory syncytical virus
RNA Viruses - drug effects
Structure-Activity Relationship
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Summary:Forty‐three 2‐[(benzotriazol‐1/2‐yl)methyl]benzimidazoles, bearing either linear (dialkylamino)alkyl‐ or bulkier (quinolizidin‐1‐yl)alkyl moieties at position 1, were evaluated in cell‐based assays for cytotoxicity and antiviral activity against viruses representative of two of the three genera of the Flaviviridae family, i.e. Flaviviruses (Yellow Fever Virus (YFV)) and Pestiviruses (Bovine Viral Diarrhoea Virus (BVDV)), as Hepaciviruses can hardly be used in routine cell‐based assays. Compounds were also tested against representatives of other virus families. Among ssRNA+ viruses were a retrovirus (Human Immunodeficiency Virus type 1 (HIV‐1)), two picornaviruses (Coxsackie Virus type B2 (CVB2), and Poliovirus type‐1, Sabin strain (Sb‐1)); among ssRNA− viruses were a Paramyxoviridae (Respiratory Syncytial Virus (RSV)) and a Rhabdoviridae (Vesicular Stomatitis Virus (VSV)) representative. Among double‐stranded RNA (dsRNA) viruses was a Reoviridae representative (Reo‐1). Two representatives of DNA virus families were also included: Herpes Simplex type 1, (HSV‐1; Herpesviridae) and Vaccinia Virus (VV; Poxviridae). Most compounds exhibited potent activity against RSV, with EC50 values as low as 20 nM. Moreover, some compounds, in particular when bearing a (quinolizidin‐1‐yl)alkyl residue, were also moderately active against BVDV, YFV, and CVB2.
ISSN:1612-1872
1612-1880
DOI:10.1002/cbdv.200890203