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Compounds, showing selectivity towards COX-2, are promising agents as selective non-steroidal anti-inflammatory drugs (NSAIDs) with lower side effects, especially, gastrointestinal ones. However, recent reports reveal the cardiovascular side effec ts associated with the selective COX-2 inhibitors. Therefore, attempts have been done to develop the second generation of selective COX-2 inheritors. They have safer profile compared to the first generation. Lumiracoxib belongs to this class of compounds. In this study, the molecular structure of the target enzymes were prepared. Library of rationally designed lumiracoxib analogues were docked.
Nowadays, glycogen synthase kinase 3 (GSK-3) inhibitors become one of the most important drug targets for the development of their selective inhibitors serving as promising drugs for the treatment of many diseases, particularly Alzheimer's disease . Targeting GSK-3 enzyme has a therapeutic importance in many diseases and is one of the valuable fields for researchers in both academic research centers and pharmaceutical companies.
The Reaction of Glycerol carried out with tow aryl halides under basic conditions (K2CO3) using 5 mol% of Pd(II)Complex as catalyst, Pd(PPh3)2Cl2. The typical reaction has been performed between glycerol and bromobenzene. This reaction is achieved in water as solvent. However, the catalyst complex does not dissolve in aqueous solutions rather it acts as heterogeneous catalyst. Therefore, it is filtrated at the end of the reaction and reused several times. Accordingly, new compound were prepared by reacting glycerol with 1-bromo-2,6-dichlorobenzene. It is anticipated that the synthesized compounds may have pharmaceutical application.
Phenol derivatives have been reacted with aryl halides under heterogeneous basic catalyst (Amberlyst-21) using 5 mol% Cu(I) Complex as catalyst, [CuClPPh3]4. The typical reaction has been performed between p-cresol and bromobenzene. This reaction is achieved in o-xylene as solvent. However, the catalyst complex does not dissolve in toluene rather it acts as heterogeneous catalyst. Therefore, it is filtrated at the end of the reaction and reused several times. Accordingly, new compounds were prepared by reacting one of the bromoaryl derivatives with paracetamol. It is anticipated that the synthesized compounds may have pharmaceutical application as non-steroidial anti-inflammatory drugs (NSAIDs).
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