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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 …

C Cusan, G Spalluto, M Prato, M Adams, A Bodensieck…

Index: Cusan, Claudia; Spalluto, Giampiero; Prato, Maurizio; Adams, Michael; Bodensieck, Antje; Bauer, Rudolf; Tubaro, Aurelia; Bernardi, Paolo; Da Ros, Tatiana Farmaco, 2005 , vol. 60, # 4 p. 327 - 332

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Citation Number: 16

Abstract

A series of acyl derivatives of 3-amino-1-phenyl-4, 5-dihydro-1H-pyrazol-5-one as potential human 5-LOX and COX 1 and COX-2 inhibitors structurally related to the 1-phenyl-3- pyrazolidinone (phenidone, 1) have been synthesized and the activity against COX-1, COX- 2 and human 5-LOX enzymes has been evaluated. All the derivatives showed poor activity against enzymes. These data, together with our previous studies, indicated that ...