Pyrazolo[3,4-d]pyrimidine derivatives as COX-2 selective inhibitors: synthesis and molecular modelling studies
| Autor: | RAFFA, Demetrio, MAGGIO, Benedetta, PLESCIA, Fabiana, CASCIOFERRO, Stella Maria, RAIMONDI, Maria Valeria, PLESCIA, Salvatore, CUSIMANO, Maria Grazia |
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| Přispěvatelé: | Raffa, D, Maggio, B, Plescia, F, Cascioferro, SM, Raimondi, MV, Plescia, S, Cusimano, MG |
| Rok vydání: | 2009 |
| Předmět: |
Models
Molecular Sulfonamides Sheep Cyclooxygenase 2 Inhibitors Indomethacin Anti-Inflammatory Agents Settore CHIM/08 - Chimica Farmaceutica Structure-Activity Relationship 4(3H)-Quinazolinone Pyrimidines Docking Pyrazolo[3 4-d]pyrimidine Cyclooxygenase 1 Animals Humans Pyrazoles Computer Simulation COX-2 inhibitor Nitrobenzenes |
| Zdroj: | Archiv der Pharmazie. 342(6) |
| ISSN: | 1521-4184 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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