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

E Perola; L Cellai; M Brufani

doi:10.1016/s0960-894x(98)00076-6

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. doi: 10.1016/s0960-894x(98)00076-6.

Authors

E Perola¹, L Cellai, M Brufani

Affiliation

¹ Istituto di Strutturistica Chimica G. Giacomello, CNR, Roma, Italy. perola@isc.mlib.cnr.it

PMID: 9871563
DOI: 10.1016/s0960-894x(98)00076-6

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.

MeSH terms

Acetamides / chemical synthesis*
Acetamides / pharmacology*
Acetylcholinesterase / metabolism
Alzheimer Disease / drug therapy
Animals
Brain / enzymology
Catalytic Domain
Cattle
Cholinesterase Inhibitors / chemical synthesis*
Cholinesterase Inhibitors / pharmacology*
Erythrocytes / enzymology
Humans
Protein Conformation
Solubility
Structure-Activity Relationship
Torpedo

Substances

Acetamides
Cholinesterase Inhibitors
Acetylcholinesterase