Author/Authors :
Cl?udio Viegas Jr.، نويسنده , , Vanderlan S. Bolzani، نويسنده , , Lu?sa S.B. Pimentel، نويسنده , , Newton G. Castro، نويسنده , , Rafael F. Cabral، نويسنده , , Rodrigo S. Costa، نويسنده , , Corinne Floyd، نويسنده , , Mônica S. Rocha، نويسنده , , Maria C.M. Young، نويسنده , , Eliezer J. Barreiro، نويسنده , , Carlos A.M. Fraga، نويسنده ,
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 μM, 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.
Keywords :
Acetylcholinesterase inhibitors , Piperidine alkaloids , Senna spectabilis , Alzheimer’s disease
