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http://dx.doi.org/10.12925/jkocs.2006.23.4.10

Synthesis of [1,2,4]-Triazole Derivatives Containing Benzimidazole and Biological Activities  

Lee, So-Ha (Life Sciences Division, Korea Institute of Science and Technology)
Jeon, Jae-Ho (Life Sciences Division, Korea Institute of Science and Technology)
Lim, Hye-Won (Life Sciences Division, Korea Institute of Science and Technology)
Pae, Ae-Nim (Life Sciences Division, Korea Institute of Science and Technology)
Publication Information
Journal of the Korean Applied Science and Technology / v.23, no.4, 2006 , pp. 355-361 More about this Journal
Abstract
[1,2,4]-Triazole derivatives were synthesized by 5 steps. Benzimidazole was refluxed with ethyl chloroacetate to give 1H-benzimidazole-acetic acid ethyl ester (1) over 52% yield. Ester (1) was refluxed with hydrazine hydrate in the presence of ethanol to afford 1H-benzimidazole-1-acetic acid, hydrazide (2). 5-Benzoimidazol-1-ylmethyl-4H-[1,2,4]triazole-3-thiol (4) was made via coupling of compound (2) with methyl isothiocyanate, followed by cyclization of 1H-benzimidazole-1-acetic acid, 2-[(methylamino) thioxomethyl]hydrazide (3) on reflux, and finally the target compounds (6a-6v) were synthesized by general substitution reaction. Compounds (6a-6v) were screened for T-type calcium channel blocker using the fluorescence assay by FDSS6000. All compounds (6a-6v) did not show better activities than control compound, mibefradil.
Keywords
benzimidazole; [1,2,4]-triazol; T-type calcium channel blocker; biological activities;
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