콘텐츠 본문
논문 해외 국제전문학술지(SCI급) DEVELOPMENT OF CHOLINESTERASE INHIBITORS USING (A)-LIPOIC ACID-BENZYL PIPERAZINE HYBRID MOLECULES
- 학술지 구분 국제전문학술지(SCI급)
- 게재년월 2013-11
- 저자명 박정호
- 학술지명 BULLETIN OF THE KOREAN CHEMICAL SOCIETY
- 발행처명 KOREAN CHEMICAL SOC
- 발행국가 해외
- 논문언어 외국어
- 전체저자수 5
논문 초록 (Abstract)
A series of hybrid molecules between (alpha)-lipoic acid (ALA) and benzyl piperazines were synthesized and their in vitro cholinester ase [acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE)] inhibitory activities were evaluated. Even though the parent co mpounds did not show any inhibitory activity against cholinesterase (Ch E), all hybrid molecules showed BuChE inhibitory activity. Some hybrid compounds also displayed AChE inhibitory activity. Specificall y, ALA-1-(3-methylbenzyl)piperazine (15) was shown to be an effec tive inhibitor of both BuChE (IC50 = 2.3 +/- 0.7 mu M) and AChE (IC 50 = 30.31 +/- 0.64 i mu M). An inhibition kinetic study using comp ound 15 indicated a mixed inhibition type. Its binding affinity (K-i) value to BuChE is 2.91 +/- 0.15 mu M.
