Author

Biblio print

Tree Display

AceDB Schema

XML Display

Feedback

Author Report for: Cabral RF

Title: New selective acetylcholinesterase inhibitors designed from natural piperidine alkaloids
Viegas C, Jr., Bolzani VS, Pimentel LS, Castro NG, Cabral RF, Costa RS, Floyd C, Rocha MS, Young MC and Fraga CA <1 more author(s)> Viegas C, Jr., Bolzani VS, Pimentel LS, Castro NG, Cabral RF, Costa RS, Floyd C, Rocha MS, Young MC, Barreiro EJ, Fraga CA (- 1)
Ref: Bioorganic & Medicinal Chemistry, 13:4184, 2005 : PubMed
Abstract


ESTHER: Viegas_2005_Bioorg.Med.Chem_13_4184
PubMedSearch: Viegas 2005 Bioorg.Med.Chem 13 4184
PubMedID: 15878668
Inhibitor(s) related to this paper: LASSBio-767, LASSBio-822

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.