Structure-based design of phthalimide derivatives as potential cyclooxygenase-2 (COX-2) inhibitors: Anti-inflammatory and analgesic activities

Anti-inflammatory and non ulcerogenic activities of acetylbergenin

“…Inhibition of COX-1 is responsible for the adverse gastrointestinal and renal effects of NSAIDs, while the inhibition of COX-2 accounts for NSAIDs therapeutic effects. All classical NSAIDs, such as aspirin and indomethacin are nonselective inhibitors of both COX-1 and COX-2, but bind more tightly to COX-1 (Alanazi et al, 2015). Chung et al (2001) reported that acetylbergenin, presented greater activity in vivo when compared with bergenin, against the hepatotoxicity in rats.…”

Design, synthesis of 2,3-disubstitued 4(3H)-quinazolinone derivatives as anti-inflammatory and analgesic agents: COX-1/2 inhibitory activities and molecular docking studies

“…Anti-inflammatory activity of the newly synthesized compounds was evaluated using the rat carrageenan-induced foot paw edema model [30][31][32] , with the use of diclofenac sodium and celecoxib as comparable reference drugs (Table 1). …”

“…The anti-inflammatory properties of the tested compounds were evaluated using an in vivo rat carrageenan-induced foot paw edema model as reported previously [30][31][32] , while the analgesic activity was examined using the hot plate method according to the previously described procedure 31,33,34 . The ED 50 for each compound was then calculated by linear regression.…”

“…Compounds exhibiting anti-inflammatory activity with ED 50 values of less than 200 mg/kg were selected for analgesic activity evaluation using the hot plate technique in mice 31,33,34 (Table 1). These compounds were found to be more active than diclofenac sodium and celecoxib (ED 50 = 100.4 and 71.0 mg/kg) after 60 minutes.…”

Design, Synthesis, Molecular Docking, and Cholinesterase Inhibitory Potential of Phthalimide‐Dithiocarbamate Hybrids as New Agents for Treatment of Alzheimer's Disease

“…The phthalimide is a bicyclic heterocyclic scaffold and its derivatives have diverse range of biologically activities such as anti‐inflammatory, anticonvulsant, hypolipidemic, analgesic, and immunomodulatory activities . Recently, several derivatives of phthalimide with high inhibitory activity against AChE have been reported ( Figure A and B ) .…”