콘텐츠 본문
논문 해외 국제전문학술지(SCI급) Tryptamine-Triazole Hybrid Compounds for Selective Butyrylcholinesterase Inhibition
- 학술지 구분 국제전문학술지(SCI급)
- 게재년월 2019-06
- 저자명 박정호
- 학술지명 BULLETIN OF THE KOREAN CHEMICAL SOCIETY
- 발행처명 WILEY-V C H VERLAG GMBH
- 발행국가 해외
- 논문언어 외국어
- 전체저자수 7
논문 초록 (Abstract)
Tryptamine-triazole hybrid compounds (11-18) were synthesized via click reaction between tryptamine azide and propargylated natural compounds. Their cholinesterase inhibitory activity was evaluated. Among the eight compounds, compound 11 showed the most potent inhibitory activity [IC50 = 0.42 +/- 0.29 mu M for equine butyrylcholinesterase (BuChE) and 1.96 +/- 0.15 mu M for human BuChE]. From the molecular modeling study, compound 11 was bound to the catalytic anionic site, anionic subsite, peripheral anionic subsite, acyl-binding pocket, and oxyanion hole of human or horse BuChE by forming a hairpin or U-shaped structure. The Lineweaver-Burk plot of compound 11 against BuChE suggests a mixed type of inhibition which corresponds well with the molecular modeling study.
