Synthesis and biological evaluation of a new class of acyl derivatives of 3-amino-1-phenyl-4,5-dihydro-1H-pyrazol-5-one as potential dual cyclooxygenase (COX-1 and COX-2) and human lipoxygenase (5-LOX) inhibitors
β Scribed by Claudia Cusan; Giampiero Spalluto; Maurizio Prato; Michael Adams; Antje Bodensieck; Rudolf Bauer; Aurelia Tubaro; Paolo Bernardi; Tatiana Da Ros
- Book ID
- 113619804
- Publisher
- Elsevier Science
- Year
- 2005
- Tongue
- English
- Weight
- 176 KB
- Volume
- 60
- Category
- Article
- ISSN
- 0014-827X
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## Abstract For Abstract see ChemInform Abstract in Full Text.
Fourteen new 3-[4-(amino/methylsulfonyl)phenyl]methylene-indolin-2-one derivatives were synthesized. Six compounds displayed potent inhibitory activities against COX-1/2 and 5-LOX with IC 50 in the range of 0.10-9.87 lM. Particularly, 10f exhibited well balanced inhibitory action on these enzymes (I
## Abstract Novel __N__βsubstitutedβ3βaminoβ5βoxoβ4βphenylβ2,5βdihydroβ1__H__βpyrazoleβ1βcarbothioamide derivatives were synthesized by means of two methods. First is the cyclization reaction of 1β(cyanophenyl)acetylβ4βsubstituted thiosemicarbazide, and the second one is reaction of cyanophenyl ace