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| Type |
Poster Presentation |
| Area |
의약화학 |
| Room No. |
포스터발표장 |
| Time |
4월 20일 (목요일) 11:00~12:30 |
| Code |
MEDI.P-441 |
| Subject |
Synthesis of Cholinesterase Inhibitor using Lipoic-benzyl triazole
Derivatives
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| Authors |
전철민*, 이하늘, 강유정, 김나연, 박정호1,*
한밭대학교 화학생명공학과, Korea
1한밭대학교 응용화학생명공학부, Korea
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| Abstract |
Alzheimer’s disease (AD) is the most common neurodegenerative disease among the cause of dementia which can appear in the elderly people aged 65 or old. The cause of Alzheimer's disease is not yet known exactly. Alzheimer's drugs based on the cholinergic theory currently marketed for the treatment of AD patient. However, they have serious side effects. We have been researching to find out new candidate compounds as cholinesterase inhibitors. In this study, a series of triazol compounds coupled by Click reaction between propagyl lipoic amide and benzyl azides were synthesized and their in vitro cholinesterase [acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE)] inhibitory activities were evaluated. Benzyl azides were selected to study the structure-activity relationship (SAR) depended on the Claig plot; plotting the sigma constants of the Hammett equation (б) versus hydrophobicity (π). The IC50 value of compound 29 (-б, -π) is 8.4±0.5μM and it is comparable to that of galantamine (IC50 = 9.4±2.5μM against BuChE). |
| E-mail |
cjfals2970@naver.com |
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119th General Meeting of the KCS