Details

Autor(en) / Beteiligte

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

Titel

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

Ist Teil von

• Bioorganic & medicinal chemistry, 2011-04, Vol.19 (8), p.2641-2649

Ort / Verlag

Amsterdam: Elsevier Ltd

Erscheinungsjahr

2011

Link zum Volltext

Quelle

Elsevier ScienceDirect Journals Complete

Beschreibungen/Notizen

• 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 (IC₅₀=1.76μg/mL) and a remarkable selectivity index (328). These compounds were selected for further evaluation as novel enterovirus inhibitors.