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(Reference retrieved automatically from Web of Science through information on FAPESP grant and its corresponding number as mentioned in the publication by the authors.)

New selective acetylcholinesterase inhibitors designed from natural piperidine alkaloids

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Author(s):
Viegas Jr, Cláudio ; Bolzani, Vanderlan S. [2] ; Pimentel, Luísa S. B. ; Castro, Newton G. ; Cabral, Rafael F. ; Costa, Rodrigo S. ; Floyd, Corinne ; Rocha, Mônica S. ; Young, Maria C. M. ; et al
Total Authors: 10
Document type: Journal article
Source: Bioorganic & Medicinal Chemistry; v. 13, n. 13, p. 4184-4190, July 2005.
Field of knowledge: Physical Sciences and Mathematics - Chemistry
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 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. (AU)

FAPESP's process: 98/05074-0 - Conservation and sustainable use of the plant biodiversity from the Cerrado and the Atlantic Forest: chemical diversity and prospecting for potential drugs
Grantee:Vanderlan da Silva Bolzani
Support type: BIOTA-FAPESP Program - Thematic Grants