New selective acetylcholinesterase inhibitors designed from natural piperidine alkaloids
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Data
2005-07-01
Autores
Viegas, C.
Bolzani, Vanderlan da Silva [UNESP]
Pimentel, LSB
Castro, N. G.
Cabral, R. F.
Costa, R. S.
Floyd, C.
Rocha, M. S.
Young, MCM
Barreiro, E. J.
Título da Revista
ISSN da Revista
Título de Volume
Editor
Elsevier B.V.
Resumo
Five new piperidine alkaloids were designed from natural (-)-3-O-acetyl-spectaline and (-)-spectaline that were obtained from the flowers of Senna spectabilis (sin. Cassia spectabilis, Leguminosae). Two semi-synthetic analogues (7 and 9) inhibited rat brain acetylcholinesterase, showing IC50 of 7.32 and 15.1 mu M, and were 21 and 9.5 times less potent against rat brain butyrylcholinesterase, respectively. Compound 9 (1 mg/kg, ip) was fully efficacious in reverting scopolamine-induced amnesia in mice. The two active compounds (7 and 9) did not show overt toxic effects at the doses tested in vivo. (c) 2005 Elsevier Ltd. All rights reserved.
Descrição
Palavras-chave
piperidine alkaloids, acetylcholinesterase inhibitors, Alzheimer's disease, Senna spectabilis
Como citar
Bioorganic & Medicinal Chemistry. Oxford: Pergamon-Elsevier B.V., v. 13, n. 13, p. 4184-4190, 2005.