ACETYLCHOLINESTERASE INHIBITION BY TACRINE ANALOGS

Authors
VALENTI P RAMPA A BISI A ANDRISANO V CAVRINI V FIN L BURIANI A GIUSTI P
Citation
P. Valenti et al., ACETYLCHOLINESTERASE INHIBITION BY TACRINE ANALOGS, Bioorganic & medicinal chemistry letters, 7(20), 1997, pp. 2599-2602
Citations number
20
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
7
Issue
20
Year of publication
1997
Pages
2599 - 2602
Database
ISI
SICI code
0960-894X(1997)7:20<2599:AIBTA>2.0.ZU;2-5
Abstract
Analogues of tacrine were synthesized and evaluated for acetylcholines terase (AChE) and butyrylcholinesterase (BuChE) inhibitory activity. C ompound 2a was the most potent inhibitor of AChE with a higher selecti vity than tacrine for AChE over BuChE. Tacrine, on the other hard, sho wed the opposite behaviour with a weaker inhibitory effect on AChE tha n on BuChe. The compounds displayed correlated activities in isolated enzymes as well as in rat brain homogenates. (C) 1997 Elsevier Science Ltd.