Carbamate analogues of (-)-physostigmine: in vitro inhibition of acetyl- and butyrylcholinesterase.
FEBS Lett
; 234(1): 127-30, 1988 Jul 04.
Article
en En
| MEDLINE
| ID: mdl-3391264
ABSTRACT
Reaction of (-)-eseroline (1) with alkyl, aryl and aralkylisocyanates afforded a series of carbamate analogues of (-)-physostigmine (2) which were assayed for inhibition of acetyl- and butyrylcholinesterase (AChE and BChE, respectively) in vitro. Included in this study were two N-alkyl-substituted carbamates 9 and 14 obtained from (-)-eseroline (1) with dialkylcarbamoyl chlorides, and allophanates 12 and 13 obtained as by-products in the reaction of 1 and benzylcarbamoyl eseroline (8) with benzyl isocyanate. Whereas none of the analogues studied was more potent than 2 against electric eel AChE, and carbamates 6, 7 and 8 were all more than 3 times more potent against human plasma BChE than 2.
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Banco de datos:
MEDLINE
Asunto principal:
Fisostigmina
/
Carbamatos
/
Inhibidores de la Colinesterasa
Límite:
Animals
/
Humans
Idioma:
En
Revista:
FEBS Lett
Año:
1988
Tipo del documento:
Article