콘텐츠 본문
논문 해외 국제전문학술지(SCI급) DEVELOPMENT OF CHOLINESTERASE INHIBITORS USING 1-BENZYL PIPERIDIN-4-YL (ALPHA)-LIPOIC AMIDE MOLECULES
- 학술지 구분 국제전문학술지(SCI급)
- 게재년월 2014-06
- 저자명 박정호
- 학술지명 BULLETIN OF THE KOREAN CHEMICAL SOCIETY
- 발행처명 KOREAN CHEMICAL SOC
- 발행국가 해외
- 논문언어 외국어
- 전체저자수 6
논문 초록 (Abstract)
A series of hybrid molecules between (alpha)-lipoic acid (ALA) and 4-amino-1-benzyl piperidines were synthesized and their in vitro cholinesterase (acetylcholinesterase (AChE) and butyrylcholinest erase (BuChE)) inhibitory activities were evaluated. Even though the p arent compounds did not exhibit any inhibitory activity against cholinesterase (ChE) withthe exception of compound 14 (I C50 = 255.26 +/- 4.41 against BuChE), all hybrid molecules demonstrate d BuChE inhibitory activity. Some hybrid compounds also displayed AChE inhibitory activity. Specifically, compound 17 was shown to be an effective inhibitor against both AChE (IC50 = 1.75 +/- 0 .30 mu M) and BuChE (IC50 = 5.61 +/- 1.25 mu M) comparable to galantam ine (IC50 = 1.7 +/- 0.9 mu M against AChE and IC50 = 9.4 +/- 2.5 mu M ag ainst BuChE). Inhibition kinetic studies using compound 17 indicated a mixed inhibition type for AChE and a noncompetitive inhibition type for BuChE. Its binding affinity (K-i) values to AChE and BuC hE were 3.8 +/- 0.005 mu M and 7.0 +/- 0.04 mu M, respectively.
