title: Inhibitory properties of 2-substituent-1H-benzimidazole-4-carboxamide derivatives against enteroviruses.
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.
authors: School of Chemistry and Chemical Engineering, Shanghai Jiaotong University, Shanghai, PR China.
authors: Fei
authors: F
authors: Xue
authors: Xianjin
authors: X
authors: Luo
authors: Chenghao
authors: C
authors: Ye
authors: Weidong
authors: W
authors: Ye
authors: Yue
authors: Y
authors: Wang
mesh_terms: D000818:Animals; D000998:Antiviral Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D001562:Benzimidazoles / Q000138:chemical synthesis / Q000494:pharmacology*; D002522:Chlorocebus aethiops; D015195:Drug Design; D004770:Enterovirus / Q000187:drug effects; D020128:Inhibitory Concentration 50; D008826:Microbial Sensitivity Tests; D013329:Structure-Activity Relationship; D014709:Vero Cells / Q000187:drug effects*
chemical_list: D000998:Antiviral Agents; D001562:Benzimidazoles