Jordi Frigola

Synthesis, structure and inhibitory effects on cyclooxygenase, lipoxygenase, thromboxane synthetase and platelet aggregation of 3-amino-4,5-dihydro-1H-pyrazole derivatives

Abstract 3-Amino-4,5-dihydro-1 H -pyrazoles ( 1–4, 7 ) and related compounds ( 5, 6 ) and some pyrazoles ( 8b–13b ) were prepared. The structures were mainly determined by 13 C NMR spectroscopy. The inhibitory activities on cyclooxygenase, 15-lipoxygenase, thromboxane synthetase and platelet aggregation were assayed. Some compounds are potent inhibitors of 15-lipoxygenase; 4,5-dihydro-3-(1-pyrrolyl)-1-(3-trifluoromethylphenyl)-1 H -pyrazole 7aw was the most potent. 7aw also had a potent inhibitory effect on cyclooxygenase and thromboxane synthetase.3-Amino-4,5-dihydro-1H-pyrazoles (1–4, 7) and related compounds (5, 6) and some pyrazoles (8b–13b) were prepared. The structures were mainly determined by 13C NMR spectroscopy. The inhibitory activities on cyclooxygenase, 15-lipoxygenase, thromboxane synthetase and platelet aggregation were assayed. Some compounds are potent inhibitors of 15-lipoxygenase; 4,5-dihydro-3-(1-pyrrolyl)-1-(3-trifluoromethylphenyl)-1H-pyrazole 7aw was the most potent. 7aw also had a potent inhibitory effect on cyclooxygenase and thromboxane synthetase.

Original paperSynthesis, structure and inhibitory effects on cyclooxygenase, lipoxygenase, thromboxane synthetase and platelet aggregation of 3-amino-4,5-dihydro-1H-pyrazole derivativesSynthèse et structure de dérivés amino-3 dihydro-4,5 1H-pyrazole; effets inhibiteurs sur la cyclooxygénase, la lipoxygénase, la thromboxane synthétase et l'agrégation plaquettaire☆

Abstract 3-Amino-4,5-dihydro-1 H -pyrazoles ( 1–4, 7 ) and related compounds ( 5, 6 ) and some pyrazoles ( 8b–13b ) were prepared. The structures were mainly determined by 13 C NMR spectroscopy. The inhibitory activities on cyclooxygenase, 15-lipoxygenase, thromboxane synthetase and platelet aggregation were assayed. Some compounds are potent inhibitors of 15-lipoxygenase; 4,5-dihydro-3-(1-pyrrolyl)-1-(3-trifluoromethylphenyl)-1 H -pyrazole 7aw was the most potent. 7aw also had a potent inhibitory effect on cyclooxygenase and thromboxane synthetase.3-Amino-4,5-dihydro-1H-pyrazoles (1–4, 7) and related compounds (5, 6) and some pyrazoles (8b–13b) were prepared. The structures were mainly determined by 13C NMR spectroscopy. The inhibitory activities on cyclooxygenase, 15-lipoxygenase, thromboxane synthetase and platelet aggregation were assayed. Some compounds are potent inhibitors of 15-lipoxygenase; 4,5-dihydro-3-(1-pyrrolyl)-1-(3-trifluoromethylphenyl)-1H-pyrazole 7aw was the most potent. 7aw also had a potent inhibitory effect on cyclooxygenase and thromboxane synthetase.