Design, synthesis and evaluation of some pyrazolo[3,4-d]pyrimidines as anti-inflammatory agents

Research developments in the syntheses, anti-inflammatory activities and structure–activity relationships of pyrimidines

“…The potency (in the form of IC 50 and SI values) of ve selected analogs (10)(11)(12)(13)(14), celecoxib, and diclofenac sodium is provided in Table 3. 78 Synthesis and anti-inammatory activities of tetrahydrobenzo [4,5]thieno [2,3-d]pyrimidine analogs have been reported. Western blotting and reverse transcription-polymerase chain reaction (RT-PCR) examinations were performed to study the inuence of the synthesized compounds on messenger ribonucleic acid (mRNA) and protein levels of iNOS and COX-2 enzyme in RAW264.7 cells.…”

Discovery and evaluation of novel synthetic 5-alkyl-4-oxo-4,5-dihydro-[1,2,4]triazolo[4,3-a]quinoxaline-1-carbox-amide derivatives as anti-inflammatory agents

“…To evaluate the anti-inflammatory activity of compound 6p in vivo, a carrageenan-induced mouse paw oedema model was used 10,26 . Each test compound (lead compound D1, 6p, and the positive controls ibuprofen and celecoxib) was administered orally at a dose of 25 mg/kg body weight prior to the induction of inflammation by carrageenan (0.1 ml) injection.…”

Pyrazolo[4,3-c]pyridine-4-one (PP-4-one) Exhibits Anti-Epileptogenic Effect in Rat Model of Traumatic Epilepsy by Mammalian Target of Rapamycin (mTOR) Signaling Pathway Downregulation

“…Pyrazole, a heterocyclic molecule, is the structural moiety in several pharmacological compounds and FDA-approved drug candidates [ 11 ]. Prominent compounds containing pyrazole include anti-inflammatory drugs (e.g., celecoxib and lonazolac), insecticides (e.g., fipronil), and analgesics (e.g., dipyrone [ 12 – 14 ]. The structure of pyrazole has received considerable interest because of its presence in compounds with a wide spectrum of pharmacological activities, such as like anti-convulsant, tranquillizing, psychoanaleptic, anti-hypotensive, and antidepressant properties [ 15 ].…”