Amnesia Research Today is a free monthly online journal that collates and summarizes the latest research about Amnesia, including details on memory loss, causes, treatment, brain injury,.

New selective acetylcholinesterase inhibitors designed from natural piperidine alkaloids.

Viegas C, Bolzani VS, Pimentel LS, Castro NG, Cabral RF, Costa RS, Floyd C, Rocha MS, Young MC, Barreiro EJ, Fraga CA

Laboratório de Avaliação e Síntese, de Substâncias Bioativas, Faculdade de Farmácia, Universidade Federal do Rio de Janeiro, CP 68023, 21944-910, Rio de Janeiro, Brazil.

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 microM, and were 21 and 9.5 times less potent against rat brain butyrylcholinesterase, respectively. Compound 9 (1mg/kg, i.p.) 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.

Published 1 June 2005 in Bioorg Med Chem, 13(13): 4184-90.
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