3, 5-Diphenyl-1H-pyrazole衍生品。1-(2-羟乙基)-3,5-二苯基- 1h -吡唑及其4-溴衍生物的酯类和n -取代氨基甲酸酯类,具有抑制、抗心律失常、镇痛等活性。

Il Farmaco; edizione scientifica Pub Date : 1988-09-01
F Bondavalli, O Bruno, A Ranise, P Schenone, P Addonizio, V De Novellis, A Loffreda, E Marmo
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引用次数: 0

摘要

描述了以环氧查尔酮为起始原料合成1-(2-羟乙基)-3,5-二苯基- 1h -吡唑(II)及其4-溴衍生物(III),以及由(II)和(III)衍生的一系列酯和n -取代氨基甲酸酯。其中部分化合物对小鼠和大鼠具有显著的抑制、抗心律失常和镇痛作用。此外,上述化合物通常在大鼠中表现出中度的降压、心动过缓和抗炎活性,在小鼠中表现出浸润麻醉和降糖活性,在体外表现出弱的血小板抗聚集活性。
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3,5-Diphenyl-1H-pyrazole derivatives. I--Esters and N-substituted carbamates of 1-(2-hydroxyethyl)-3,5-diphenyl-1H-pyrazole and its 4-bromo derivative with depressant, antiarrhythmic, analgesic and other activities.

The synthesis of 1-(2-hydroxyethyl)-3,5-diphenyl-1H-pyrazole (II) and its 4-bromo derivative (III) starting from chalcone epoxide, as well as of a series of esters and N-substituted carbamates derived from (II) and (III), is described. Some of these compounds showed remarkable depressant, antiarrhythmic and analgesic activities in mice and rats. Moreover, the above compounds usually exhibited moderate hypotensive, bradycardic and antiinflammatory activities in rats, infiltration anesthesia and hypoglycemic activity in mice, as well as a weak platelet antiaggregating activity in vitro.

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