Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
7803094 | European Journal of Medicinal Chemistry | 2011 | 15 Pages |
Abstract
⺠Quinolizidinyl derivatives of bi- and tricyclic systems potently inhibit AChE and/or BChE. ⺠The thioxanthene derivative 15 inhibits preferentially BChE (IC50 = 0.15 μM, SI = 47). ⺠The acridine derivative 43 is a balanced AChE/BChE inhibitor (IC50 = 0.22 and 0.69 μM respectively). ⺠The 6-hydroxy coumarine derivative 46 inhibits preferentially AChE (IC50 = 0.35 μM, SI = 15). ⺠Remarkably periciazine 3 potently inhibits BChE (IC50 = 0.23 μM), many fold more than the common anti-psychotics.
Keywords
NMDAtorpedo californica acetylcholinesterase5,5-dithiobis(2-nitrobenzoic acid)Quinolizidine derivativesTcAChEBChEN-methyl-d-aspartatebutyrylcholinesteraseADMEDTNBAββ-AmyloidAChAChEAcetylcholineAcetylcholinesteraseAlzheimer’s diseaseabsorption, distribution, metabolism and excretionPeripheral anionic siteselectivity indexButyrylcholinesterase inhibitorsacetylcholinesterase inhibitorsPASHydrogen bondCHECholinesterase
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
B. Tasso, M. Catto, O. Nicolotti, F. Novelli, M. Tonelli, I. Giangreco, L. Pisani, A. Sparatore, V. Boido, A. Carotti, F. Sparatore,