Nowadays, the usage of NSAIDs has been increased dramatically
for relieving pain and the treatment of divers inflammatory
conditions, therefore, it is necessary to develop this class of drug
by increasing their activity and decreasing their side e
ffects. Their
most common side effect is the gastrointestinal disorders,
especially, gastric bleeding resulting from the inhibition of
prostaglandins synthesis.
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.
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.