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제125회 대한화학회 학술발표회 및 총회 Investigation of inhibitory effect of 7-azaindoles derivatives against cholinesterase activity

등록일
2020년 2월 6일 16시 35분 20초
접수번호
1164
발표코드
MEDI.P-707 이곳을 클릭하시면 발표코드에 대한 설명을 보실 수 있습니다.
발표시간
온라인 PDF 제출
발표형식
포스터
발표분야
Medicinal Chemistry
저자 및
공동저자
Kooyeon Lee*, Jeong Ju Oh
Department of Bio-Health Technology, Kangwon National University, Korea
Cholinesterases including acetylcholinesterase and butyrylcholinesterase have emerged as a molecular target to treat Alzheimer’s disease; however, development of molecules inhibiting simultaneously two cholinesterases has been limited. To discover novel molecules simultaneously inhibiting cholinesterases, we synthesized 7-azaindole derivatives because the azaindole moiety has a number of useful biological activities. 7-Azaindole derivatives are synthesized through base-mediated Michael addition of carbon nucleophiles to 3-(1-arylsulfonylalkyl)-7-azaindole. 18 chemical structures with 7-azaindole scaffold were confirmed 1H NMR. The inhibitory effects of various derivatives on cholinesterases were determined by calculating the half maximal inhibitory concentrations (IC50). Most derivatives showed dose-dependent decrease of both cholinesterases activities. Particularly, 2-((3-nitrophenyl)(1H-pyrrolo[2,3-b]pyridin-3-yl)methyl)malononitrile exhibited significant inhibitory effect against acetylcholinesterase activity with IC50 value of 7.04 μM. Thus, this study may be useful for developing potential drugs for treating Alzheimer’s disease.

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