6533b852fe1ef96bd12abd76
RESEARCH PRODUCT
Pyrazolo[3,4-d]pyrimidine derivatives as COX-2 selective inhibitors: synthesis and molecular modelling studies.
Demetrio RaffaBenedetta MaggioFabiana PlesciaStella Maria CascioferroMaria Valeria RaimondiSalvatore PlesciaMaria Grazia Cusimanosubject
Models MolecularSulfonamidesSheepCyclooxygenase 2 InhibitorsIndomethacinAnti-Inflammatory AgentsSettore CHIM/08 - Chimica FarmaceuticaStructure-Activity Relationship4(3H)-QuinazolinonePyrimidinesDocking Pyrazolo[34-d]pyrimidineCyclooxygenase 1AnimalsHumansPyrazolesComputer SimulationCOX-2 inhibitorNitrobenzenesdescription
The pyrazolo[3,4-d]pyrimidine system shows a multitude of interesting pharmacological properties. Owing to the potential anti-inflammatory activity of 5-benzamido-pyrazolo[3,4-d]pyrimidin- 4-one derivatives and considering the easy synthesis of this class of compounds, a set of new 5- benzamido-1H-pyrazolo[3,4-d]pyrimidin-4-ones has been prepared in 42-80% yields by reacting 5- aminopyrazole-4(N-benzoyl)carbohydrazide derivatives and the opportune triethylorthoesters. Compounds 8a, b, 10a–d, and 11a, b revealed a superior inhibitory profile against COX-2, when compared to that of reference standards NS398 and indomethacin. Molecular modelling studies confirmed the obtained biological results.
| year | journal | country | edition | language |
|---|---|---|---|---|
| 2009-05-30 | Archiv der Pharmazie |