콘텐츠 본문
논문 국내 국내전문학술지(KCI급) SYNTHESIS AND IN VITRO ASSAY OF NEW TRIAZOLE LINKED DECURSINOL DERIVATIVES SHOWING INHIBITORY ACTIVITY AGAINST CHOLINESTERASE FOR ALZHEIMER’S DISEASE THERAPEUTICS
- 학술지 구분 국내전문학술지(KCI급)
- 게재년월 2016-04
- 저자명 박정호
- 학술지명 대한화학회지
- 발행처명 대한화학회
- 발행국가 국내
- 논문언어 외국어
- 전체저자수 5
논문 초록 (Abstract)
With the goal of developing Alzheimer’s disease therapeutics, we have designed and synthesized new triazole linked decursinol derivatives having potency inhibitory activities against cholinesterase [acetylcholinesterase (AChE) and butyrylcholinesterase (BuC hE)]. Since inhibition of cholinesterase (ChE) is still considered to b e one of the most effective targets totreat AD patients, many new class es of ChE inhibitors have been synthesized. In an effort of identifyi ng new type of cholinergic drug, decursinol derivatives 11-17 have been synthesized between decursinol and other biological interesting compoun ds such as lipoic acid, polyphenols, etc by using the click reaction a nd then evaluated their biological activities. Compound 12 (IC50 = 5.89 ± 0.31 mM against BuChE) showed more effective inhibitory activit y against BuChE than galantamine (IC50 = 9.4�2.5 mM). Decursinol derivatives can be considered a new class inhibitor for BuChE and can be applied to be a novel drug candidate to treat AD patients.
