Yu_2010_Bioorg.Med.Chem.Lett_20_3254

Reference

Title : Synthesis of 4-[(diethylamino)methyl]-phenol derivatives as novel cholinesterase inhibitors with selectivity towards butyrylcholinesterase - Yu_2010_Bioorg.Med.Chem.Lett_20_3254
Author(s) : Yu L , Cao R , Yi W , Yan Q , Chen Z , Ma L , Peng W , Song H
Ref : Bioorganic & Medicinal Chemistry Lett , 20 :3254 , 2010
Abstract :

A series of novel cholinesterase inhibitors, being composed of 4-[(diethylamino)methyl]-phenoxy and secondary amine which were linked with a different length alkyl chain, were designed and synthesized from the starting material p-hydroxybenzaldehyde. These compounds were evaluated as acetylcholinesterase and butyrylcholinesterase (AChE/BChE) inhibitors. Compounds 25-31 having a secondary amine moiety connected to the phenyl ring via eight CH(2) units spacer were found to be the most potent inhibitors with IC(50) value lower than 220nM and 48nM against AChE and BChE, respectively. Interestingly, these inhibitors showed a surprising selectively toward BChE, and compounds 26, 27, and 30 displayed 12.5, 18.6, and 18.8-fold higher affinity to BChE. The inhibition kinetics analyzed by Linewear-Burk plots revealed that such compounds were mix-type inhibitors.

PubMedSearch : Yu_2010_Bioorg.Med.Chem.Lett_20_3254
PubMedID: 20452769

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Citations formats

Yu L, Cao R, Yi W, Yan Q, Chen Z, Ma L, Peng W, Song H (2010)
Synthesis of 4-[(diethylamino)methyl]-phenol derivatives as novel cholinesterase inhibitors with selectivity towards butyrylcholinesterase
Bioorganic & Medicinal Chemistry Lett 20 :3254

Yu L, Cao R, Yi W, Yan Q, Chen Z, Ma L, Peng W, Song H (2010)
Bioorganic & Medicinal Chemistry Lett 20 :3254