| Title : Synthesis and Screening for Antiacetylcholinesterase Activity of (1-Benzyl-4-oxopiperidin-3-ylidene)methylindoles and -pyrroles Related to Donepezil - Andreani_2001_J.Med.Chem_44_4011 |
| Author(s) : Andreani A , Cavalli A , Granaiola M , Guardigli M , Leoni A , Locatelli A , Morigi R , Rambaldi M , Recanatini M , Roda A |
| Ref : Journal of Medicinal Chemistry , 44 :4011 , 2001 |
|
Abstract :
The design, synthesis, and rapid evaluation of a new class of acetylcholinesterase (AChE) inhibitors related to donepezil are reported. A molecular dynamics simulation of the complex between AChE and one representative compound of the series showed a possible inhibitor binding mode in which favorable interactions are formed between the benzylpiperidinone moiety and some active-site residues. The biochemical evaluation of this newly synthesized series was performed using a chemiluminescent method suitable for high-throughput screening. |
| PubMedSearch : Andreani_2001_J.Med.Chem_44_4011 |
| PubMedID: 11689088 |
Andreani A, Cavalli A, Granaiola M, Guardigli M, Leoni A, Locatelli A, Morigi R, Rambaldi M, Recanatini M, Roda A (2001)
Synthesis and Screening for Antiacetylcholinesterase Activity of (1-Benzyl-4-oxopiperidin-3-ylidene)methylindoles and -pyrroles Related to Donepezil
Journal of Medicinal Chemistry
44 :4011
Andreani A, Cavalli A, Granaiola M, Guardigli M, Leoni A, Locatelli A, Morigi R, Rambaldi M, Recanatini M, Roda A (2001)
Journal of Medicinal Chemistry
44 :4011