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.
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.
Perola
E
E
Istituto di Strutturistica Chimica G. Giacomello, CNR, Roma, Italy. perola@isc.mlib.cnr.it
Cellai
L
L
Brufani
M
M
D000081:Acetamides / Q000138:chemical synthesis* / Q000494:pharmacology*; D000110:Acetylcholinesterase / Q000378:metabolism; D000544:Alzheimer Disease / Q000188:drug therapy; D000818:Animals; D001921:Brain / Q000201:enzymology; D020134:Catalytic Domain; D002417:Cattle; D002800:Cholinesterase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D004912:Erythrocytes / Q000201:enzymology; D006801:Humans; D011487:Protein Conformation; D012995:Solubility; D013329:Structure-Activity Relationship; D014101:Torpedo
D000081:Acetamides; D002800:Cholinesterase Inhibitors; D000110:Acetylcholinesterase