Inhibitory properties of 2-substituent-1H-benzimidazole-4-carboxamide derivatives against enteroviruses

Bioorg Med Chem. 2011 Apr 15;19(8):2641-9. doi: 10.1016/j.bmc.2011.03.007.

Fei Xue ¹, Xianjin Luo, Chenghao Ye, Weidong Ye, Yue Wang

Affiliations

Affiliation

1 School of Chemistry and Chemical Engineering, Shanghai Jiaotong University, Shanghai, PR China.

PMID: 21441033 DOI: 10.1016/j.bmc.2011.03.007

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.

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