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Inhibitory properties of 2-substituent-1H-benzimidazole-4-carboxamide derivatives against enteroviruses
April 2011
April 2011
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Abstract
A series of novel benzimidazole derivatives were designed, synthesized, and evaluated
for their activities against four kinds of enteroviruses, that is, Coxsackie virus
A16, B3, B6 and Enterovirus 71 in VERO cells. Strong activities against enterovirus
replication and low cytotoxicities were observed in these benzimidazoles generally.
The most promising compound was (l)-2-(pyridin-2-yl)-N-(2-(4-nitrophenyl)pentan-3-yl)-1H-benzimidazole-4-carboxamide
(16), with a high antiviral potency (IC(50)=1.76 μg/mL) and a remarkable selectivity
index (328). These compounds were selected for further evaluation as novel enterovirus
inhibitors.