3,5-Diphenyl-1H-pyrazole derivatives. II--N-substituted 1-(2-aminoethyl)-3,5-diphenyl-1H-pyrazoles and their 4-bromo derivatives with analgesic and other activities.

Il Farmaco; edizione scientifica Pub Date : 1988-12-01
F Bondavalli, O Bruno, A Ranise, P Schenone, S Russo, A Loffreda, V De Novellis, C Lo Sasso, E Marmo
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Abstract

The synthesis of N-substituted 1-(2-aminoethyl)-3,5-diphenyl-1H-pyrazoles and their 4-bromo derivatives (V) by reaction of primary and secondary amines with the tosylates of 1-(2-hydroxyethyl)-3,5-diphenyl-1H-pyrazole and its 4-bromo derivative is described. Some of compounds (V) showed a remarkable analgesic activity in mice. Moreover, the above compounds usually exhibited moderate hypotensive, bradycardiac and antiinflammatory activities in rats, infiltration anesthesia in mice, as well as a weak platelet antiaggregating activity in vitro.

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3, 5-Diphenyl-1H-pyrazole衍生品。具有镇痛和其他活性的II- n -取代1-(2-氨基乙基)-3,5-二苯基- 1h -吡唑及其4-溴衍生物。
介绍了伯胺和仲胺与1-(2-羟乙基)-3,5-二苯基- 1h -吡唑及其4-溴衍生物的甲磺酸盐反应合成n -取代的1-(2-氨基乙基)-3,5-二苯基- 1h -吡唑及其4-溴衍生物(V)。部分化合物(V)对小鼠有明显的镇痛作用。此外,上述化合物通常在大鼠中表现出中度降压、心动过缓和抗炎活性,在小鼠中表现出浸润麻醉,在体外表现出弱的血小板抗聚集活性。
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