| Title : New selective acetylcholinesterase inhibitors designed from natural piperidine alkaloids - Viegas_2005_Bioorg.Med.Chem_13_4184 |
| 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 |
| Ref : Bioorganic & Medicinal Chemistry , 13 :4184 , 2005 |
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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. |
| PubMedSearch : Viegas_2005_Bioorg.Med.Chem_13_4184 |
| PubMedID: 15878668 |
| Inhibitor | LASSBio-767 LASSBio-822 |
Viegas C, Jr., Bolzani VS, Pimentel LS, Castro NG, Cabral RF, Costa RS, Floyd C, Rocha MS, Young MC, Barreiro EJ, Fraga CA (2005)
New selective acetylcholinesterase inhibitors designed from natural piperidine alkaloids
Bioorganic & Medicinal Chemistry
13 :4184
Viegas C, Jr., Bolzani VS, Pimentel LS, Castro NG, Cabral RF, Costa RS, Floyd C, Rocha MS, Young MC, Barreiro EJ, Fraga CA (2005)
Bioorganic & Medicinal Chemistry
13 :4184