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Benzimidazole을 함유한 [1,2,4]-Triazole 유도체의 합성 및 생물학적 활성 KCI 등재

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

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한국응용과학기술학회지 (The Korean Society of Applied Science and Technology)
한국응용과학기술학회(구 한국유화학회) (The Korean Society of Applied Science and Technology (KSAST))
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.

저자
  • 이소하 | Lee, So-Ha
  • 전제호 | Jeon, Jae-Ho
  • 임혜원 | Lim, Hye-Won
  • 배애님 | Pae, Ae-Nim