BackgroundThe evaluation of the clinical effects of Tacrine has shown efficacy in delaying the deterioration of the symptoms of Alzheimer’s disease, while confirming the adverse events consisting mainly in the elevated liver transaminase levels. The study of tacrine analogs presents a continuous interest, and for this reason we establish Quantitative Structure-Activity Relationships on their Acetylcholinesterase inhibitory activity.ResultsTen groups of new developed Tacrine-related inhibitors are explored, which have been experimentally measured in different biochemical conditions and AChE sources. The number of included descriptors in the structure-activity relationship is characterized by ‘Rule of Thumb’. The 1502 applied molecular descriptors could provide the best linear models for the selected Alzheimer’s data base and the best QSAR model is reported for the considered data sets.ConclusionThe QSAR models developed in this work have a satisfactory predictive ability, and are obtained by selecting the most representative molecular descriptors of the chemical structure, represented through more than a thousand of constitutional, topological, geometrical, quantum-mechanical and electronic descriptor types.Electronic supplementary materialThe online version of this article (doi:10.1186/s12929-014-0084-0) contains supplementary material, which is available to authorized users.
In a fluidized bed, particles of different size are subject to a force imbalance that promotes segregation. However, in conventional gas‐fluidized systems this tendency is masked by the high solids mixing rates that exist. The addition of packing or baffles permits the use of high aspect ratios and also restricts large‐scale solids movement. As a result, segregation is more pronounced. Experiments have been carried out to assess the extent of segregation occurring in gas‐fluidized systems containing an open‐ended cylindrical screen packing. The degree of segregation has been found to depend on gas flow rate and bed height. Some rate studies have also been made.
This article reviews multi-criteria QSAR applications on Acetylcholinesterase inhibitors as palliative drugs for Alzheimer's Disease, published in the period 2001-2011. It includes QSAR models for different series of compounds, comparative studies, and advances in methodologies. This period is marked by a shift in focus from palliative treatment to pathogenesis. However, we believe that research into palliative treatment should continue. More comparative studies are desirable. In order to facilitate comparative and general studies on Acetylcholinesterase inhibitors, a standard experimental protocol for measuring an inhibitor's potency is needed. Finally, we recommend chemists to work closely with system and molecular biologists.
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