Antiviral activity of benzimidazole derivatives. I. Antiviral activity of 1-substituted-2-[(benzotriazol-1/2-yl)methyl]benzimidazoles.
作者： Michele Tonelli , Giuseppe Paglietti , Vito Boido , Fabio Sparatore , Fabio Marongiu
关键词:
摘要: 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 the three genera Flaviviridae family, i.e. Flaviviruses (Yellow Fever Virus (YFV)) Pestiviruses (Bovine Viral Diarrhoea (BVDV)), as Hepaciviruses can hardly be used routine assays. Compounds also tested representatives other virus families. Among ssRNA+ a retrovirus (Human Immunodeficiency type 1 (HIV-1)), picornaviruses (Coxsackie B2 (CVB2), Poliovirus type-1, Sabin strain (Sb-1)); among ssRNA- Paramyxoviridae (Respiratory Syncytial (RSV)) Rhabdoviridae (Vesicular Stomatitis (VSV)) representative. double-stranded RNA (dsRNA) was Reoviridae (Reo-1). Two DNA families included: Herpes Simplex (HSV-1; Herpesviridae) Vaccinia (VV; Poxviridae). Most compounds exhibited potent RSV, with EC(50) values low 20 nM. Moreover, some compounds, particular when residue, moderately active BVDV, YFV, CVB2.
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