| Title : Design, synthesis, and bioevaluation of benzamides: novel acetylcholinesterase inhibitors with multi-functions on butylcholinesterase, Abeta aggregation, and beta-secretase - Peng_2012_Bioorg.Med.Chem_20_6739 |
| Author(s) : Peng DY , Sun Q , Zhu XL , Lin HY , Chen Q , Yu NX , Yang WC , Yang GF |
| Ref : Bioorganic & Medicinal Chemistry , 20 :6739 , 2012 |
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Abstract :
Alzheimer's disease (AD) is a multifactorial syndrome with several target proteins contributing to its etiology. In this study, we conducted a structure-based design and successfully produced a series of new multi-site AChE inhibitors with a novel framework. Compound 2e, characterized by a central benzamide moiety linked to an isoquinoline at one side and acetophenone at the other, was the most potent candidate with K(i) of 6.47nM against human AChE. Particularly, it showed simultaneous inhibitory effects against BChE, Abeta aggregation, and beta-secretase. We therefore conclude that compound 2e is a very promising multi-function lead for the treatment of AD. |
| PubMedSearch : Peng_2012_Bioorg.Med.Chem_20_6739 |
| PubMedID: 23041347 |
Peng DY, Sun Q, Zhu XL, Lin HY, Chen Q, Yu NX, Yang WC, Yang GF (2012)
Design, synthesis, and bioevaluation of benzamides: novel acetylcholinesterase inhibitors with multi-functions on butylcholinesterase, Abeta aggregation, and beta-secretase
Bioorganic & Medicinal Chemistry
20 :6739
Peng DY, Sun Q, Zhu XL, Lin HY, Chen Q, Yu NX, Yang WC, Yang GF (2012)
Bioorganic & Medicinal Chemistry
20 :6739