Design, Synthesis and Evaluation of Difunctionalized 4-Hydroxybenzaldehyde Derivatives as Novel Cholinesterase Inhibitors
-
- Yu Liang
- School of Chemistry and Chemical Engineering, Sun Yat-sen University
-
- Cao Rihui
- School of Chemistry and Chemical Engineering, Sun Yat-sen University
-
- Yi Wei
- School of Chemistry and Chemical Engineering, Sun Yat-sen University
-
- Yan Qin
- School of Chemistry and Chemical Engineering, Sun Yat-sen University
-
- Chen Zhiyong
- School of Chemistry and Chemical Engineering, Sun Yat-sen University
-
- Ma Lin
- School of Chemistry and Chemical Engineering, Sun Yat-sen University
-
- Song Huacan
- School of Chemistry and Chemical Engineering, Sun Yat-sen University
Search this article
Abstract
A series of difunctionalized 4-hydroxybenzaldehyde derivatives were designed, synthesized and evaluated as cholinesterase (acetylcholinesterase (AChE) and butyrylcholinesterase (BChE)) inhibitors. The results demonstrated that all the compounds had more potent AChE and BChE inhibitory activities than galanthamine-HBr, one of the best cholinesterase inhibitors known so far. The inhibition mechanism revealed that the best active compound 4e displayed a mix-type mode of AChE and BChE by its dual-site interactions with the catalytic triad active center and the peripheral anionic site (PAS) of enzyme. All these data suggested that further development of such compounds may be of interest.
Journal
-
- Chemical and Pharmaceutical Bulletin
-
Chemical and Pharmaceutical Bulletin 58 (9), 1216-1220, 2010
The Pharmaceutical Society of Japan
- Tweet
Details 詳細情報について
-
- CRID
- 1390282679149640064
-
- NII Article ID
- 130000324597
-
- NII Book ID
- AA00602100
-
- ISSN
- 13475223
- 00092363
-
- NDL BIB ID
- 10796464
-
- Text Lang
- en
-
- Data Source
-
- JaLC
- NDL
- Crossref
- CiNii Articles
-
- Abstract License Flag
- Disallowed