| Literature DB >> 15878668 |
Cláudio Viegas1, Vanderlan S Bolzani, Luísa S B Pimentel, Newton G Castro, Rafael F Cabral, Rodrigo S Costa, Corinne Floyd, Mônica S Rocha, Maria C M Young, Eliezer J Barreiro, Carlos A M Fraga.
Abstract
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.Entities:
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Year: 2005 PMID： 15878668 DOI： 10.1016/j.bmc.2005.04.030
Source DB: PubMed Journal: Bioorg Med Chem ISSN： 0968-0896 Impact factor: 3.641