Synthesis and Biological Evaluation of Novel Benzimidazole Derivatives Bearing a Heterocyclic Ring at 4/5 Position 


Vol. 34,  No. 8, pp. 2297-2304, Aug.  2013
10.5012/bkcs.2013.34.8.2297


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  Abstract

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 (IC50 = 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.

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  Cite this article

[IEEE Style]

R. Wubulikasimu, Y. Yang, F. Xue, X. Luo, D. Shao, Y. Li, R. Gao, W. Ye, "Synthesis and Biological Evaluation of Novel Benzimidazole Derivatives Bearing a Heterocyclic Ring at 4/5 Position," Bulletin of the Korean Chemical Society, vol. 34, no. 8, pp. 2297-2304, 2013. DOI: 10.5012/bkcs.2013.34.8.2297.

[ACM Style]

Reyila Wubulikasimu, Yanbing Yang, Fei Xue, Xianjin Luo, Dongping Shao, Yuhuan Li, Rongmei Gao, and Weidong Ye. 2013. Synthesis and Biological Evaluation of Novel Benzimidazole Derivatives Bearing a Heterocyclic Ring at 4/5 Position. Bulletin of the Korean Chemical Society, 34, 8, (2013), 2297-2304. DOI: 10.5012/bkcs.2013.34.8.2297.

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ISSN(Print) 0253-2964
ISSN(Online) 1229-5949