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

• 영문명: Synthesis of [1,2,4]-Triazole Derivatives Containing Benzimidazole and Biological Activities
• 발행기관: 한국응용과학기술학회 (구.한국유화학회)
• 저자명: 이소하(Lee SoHa) 전제호(Jeon JaeHo) 임혜원(Lim HyeWon) 배애님(Pae AeNim)
• 간행물 정보: 『한국응용과학기술학회지』한국유화학회지 제23권 제4호, 355~361쪽, 전체 7쪽
• 주제분류: 공학 > 화학공학
• 파일형태: PDF
• 발행일자: 2006.12.31

영문 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.

키워드

benzimidazole [1,2,4]-triazol T-type calcium channel blocker biological activities