Background: New N-substituted 5-(oxoindolinyl)-2-thioxo- thiazolidinone derivatives
Materials and Methods: The C2
-substituted thiazolidinone derivatives with piperidinyl and morpholinyl
moieties in addition to the tetracyclic [(oxindolo)pyrazino]thiazolidine, the chloro- and aminoderivatives
of the (indolyl)thiazolidinone ring system were also prepared.
Results: The COX-2 inhibition activity of the synthesized compounds was investigated by studying
their ability to inhibit the conversion of arachidonic acid to prostaglandin H2 (PGH2). Five of the
tested candidates, substituted (oxonidolyl)thiazolidine derivatives (3a, 6f, 8b, 10 and 12) showed
significant COX-2 inhibitory activity exhibiting IC50 values better than or close to the reference
celecoxib. The anti-inflammatory activity was studied revealing that a number of compounds have
shown good activities and compound 10 produced no significant mucosal injury.
Conclusion: Molecular docking study was implemented to interpret the variable inhibitory activity of
the newly synthesized compounds against COX enzyme. The results suggested that some of these
derivatives could be active COX inhibitors possessing a high preference for COX-2.