Synthesis and activity studies of N-[omega-N'-(adamant-1'-yl)aminoalkyl]- 2-(4'-dimethylaminophenyl)acetamides: in the search of selective inhibitors for the different molecular forms of acetylcholinesterase.

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Perola E, Cellai L, Brufani M

Synthesis and activity studies of N-[omega-N'-(adamant-1'-yl)aminoalkyl]- 2-(4'-dimethylaminophenyl)acetamides: in the search of selective inhibitors for the different molecular forms of acetylcholinesterase.

Bioorg Med Chem Lett. 1998 Mar 17;8(6):575-80.

PubMed ID
9871563 [ View in PubMed
]
Abstract

A series of N-[omega-N'-(adamant-1'-yl)aminoalkyl]-2-(4'- dimethylaminophenyl)acetamides were synthesized and tested as acetylcholinesterase inhibitors. A significant selectivity toward acetylcholinesterases from various natural sources, mainly differing in their quaternary structure and solubility, was pointed out. The interest of this kind of molecules as potential therapeutic agents for Alzheimer's disease is discussed.

DrugBank Data that Cites this Article

Binding Properties
DrugTargetPropertyMeasurementpHTemperature (°C)
DonepezilAcetylcholinesteraseIC 50 (nM)8N/AN/ADetails
DonepezilAcetylcholinesteraseIC 50 (nM)12N/AN/ADetails
DonepezilAcetylcholinesteraseIC 50 (nM)17N/AN/ADetails
PhysostigmineAcetylcholinesteraseIC 50 (nM)47N/AN/ADetails
PhysostigmineAcetylcholinesteraseIC 50 (nM)46N/AN/ADetails