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EnglishAP2238 was the first compound published to bind both anionic sites of the human acetylcholinesterase, allowing the simultaneous inhibition of the catalytic and the amyloid-beta pro-aggregating activities of AChE. Here we attempted to derive a comprehensive structure-activity relationship picture for this molecule, affording 28 derivatives for which AChE and BChE inhibitory activities were evaluated. Selected compounds were also tested for their ability to prevent the AChE-induced Abeta-aggregation. Moreover, docking simulations and molecular orbital calculations were performed.
| Titolo: | Extensive SAR and computational studies of 3-{4-[(benzylmethylamino)methyl]phenyl}-6,7-dimethoxy-2H-2-chromenone (AP2238) derivatives. |
| Autore/i: | PIAZZI, LORNA; CAVALLI, ANDREA; BELLUTI, FEDERICA; BISI, ALESSANDRA; GOBBI, SILVIA; Rizzo S.; BARTOLINI, MANUELA; ANDRISANO, VINCENZA; RECANATINI, MAURIZIO; RAMPA, ANGELA |
| Autore/i Unibo: | |
| Anno: | 2007 |
| Rivista: | |
| Digital Object Identifier (DOI): | http://dx.doi.org/10.1021/jm070100g |
| Abstract: | AP2238 was the first compound published to bind both anionic sites of the human acetylcholinesterase, allowing the simultaneous inhibition of the catalytic and the amyloid-beta pro-aggregating activities of AChE. Here we attempted to derive a comprehensive structure-activity relationship picture for this molecule, affording 28 derivatives for which AChE and BChE inhibitory activities were evaluated. Selected compounds were also tested for their ability to prevent the AChE-induced Abeta-aggregation. Moreover, docking simulations and molecular orbital calculations were performed. |
| Data prodotto definitivo in UGOV: | 2007-09-29 16:23:08 |
| Appare nelle tipologie: | 1.01 Articolo in rivista |
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