한국응용과학기술학회지 (Journal of the Korean Applied Science and Technology)

  • 제23권4호
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  • Pages.355-361
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  • 2006
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  • 1225-9098(pISSN)
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  • 2288-1069(eISSN)
한국응용과학기술학회 (The Korean Society of Applied Science and Technology)
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Benzimidazole을 함유한 [1,2,4]-Triazole 유도체의 합성 및 생물학적 활성

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

  • 이소하 (한국과학기술연구원 생체과학연구부) ;
  • 전제호 (한국과학기술연구원 생체과학연구부) ;
  • 임혜원 (한국과학기술연구원 생체과학연구부) ;
  • 배애님 (한국과학기술연구원 생체과학연구부)
  • 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)
  • 발행 : 2006.12.31
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초록

[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.

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참고문헌

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