A series of novel benzimidazole derivatives bearing a heterocyclic ring as oxadiazole (21-32), thiadiazole (33-34), triazole (35-36) were synthesized and evaluated for their activities against Coxsackie virus B3 and B6 in Vero cells. Compounds 21-26, 31-36 with moieties of 2'-pyridyl, 3'-pyridyl and 4'-pyridyl at the 2-position and oxadiazoles, thiadiazole, or triazole substituent at the 4-or 5-position generally displayed activities against CVB3 and CVB6. Especially compound 24 (IC 50 = 1.08 µg/mL, SI = 61.7 against CVB3) was the promising candidate as lead compound for anti-enteroviral drug. It was observed in the incorporation of heterocyclic rings in benzimidazole at the 5-position could enhance their biological activities.
The synthesis of a range of benzimidazole derivatives bearing heterocyclic rings is described by the employment of benzimidazole‐4/5‐carboxylic acid derivatives as substrates.
A series of 1,2,4-triazole derivatives were synthesized, and their abilities to inhibit the in vitro replication of Coxsackie B3/B6 were evaluated. Among the 1,2,4-triazole derivatives, compound 3 g displayed potent activity, with a high antiviral potency (IC50=1.71μM(against CVB3), 1.43μM (against CVB6)).The structures of all the new synthesized compounds were confirmed by 1H-NMR spectra,mass spectra and elemental analyses.
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