N-Acyl-N-phenyl ureas of piperidine and substituted piperidines endowed with anti-inflammatory and anti-proliferative activities
| Autor: | Angelo Ranise, Barbara Rivaldi, Olga Bruno, Francesco Bondavalli, Giuseppe Falcone, Silvia Schenone, Walter Filippelli |
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| Rok vydání: | 2001 |
| Předmět: |
Male
Cell growth Chemistry Stereochemistry medicine.drug_class Anti-Inflammatory Agents Pharmaceutical Science Anti proliferative Chemical synthesis In vitro Anti-inflammatory chemistry.chemical_compound Broad spectrum Piperidines Oral administration Drug Discovery Tumor Cells Cultured medicine Animals Humans Female Piperidine Analgesia |
| Zdroj: | Il Farmaco. 56:647-657 |
| ISSN: | 0014-827X |
| Popis: | Six series of N -acyl- N -phenyl ureas 1 – 6 of piperidine ( 1 ), and 2-ethyl- ( 2 ), 3-methyl- ( 3 ), 4-methyl- ( 4 ), 4-phenyl- ( 5 ), cis -2,6-dimethyl- ( 6 ) piperidine were synthesised and evaluated for their anti-inflammatory, anaesthetic, anti-pyretic properties. Some derivatives of series 1 and 5 were also assayed for anti-proliferative activity. Several compounds showed an anti-inflammatory activity comparable or slighty inferior to that of indomethacin in rats ( 1c , d , 2a , b , g , h , 3b , 4h , 5d , e ). Moreover, an appreciable anti-inflammatory activity was also found in 2c , e , 3e , f , g , 4g , 5a , b , c , f , h , and 6a , b , d . All the compounds were devoid of anti-pyretic activity and only a few of them exhibited a low level of infiltration anaesthesia in mice. Compound 5a showed a broad spectrum anti-cancer activity (at low micromolar concentrations), particulary significant against leukemia subpanel. |
| Databáze: | OpenAIRE |
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