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3,5-二苯基-1H-吡唑衍生物。II-N-取代的1-(2-氨基乙基)-3,5-二苯基-1H-吡唑及其具有镇痛和其他活性的4-溴衍生物。

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.

作者信息

Bondavalli F, Bruno O, Ranise A, Schenone P, Russo S, Loffreda A, De Novellis V, Lo Sasso C, Marmo E

机构信息

Istituto di Scienze Farmaceutiche, Università di Genova, Italy.

出版信息

Farmaco Sci. 1988 Dec;43(12):1019-34.

PMID:3248592
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.

摘要

描述了通过伯胺和仲胺与1-(2-羟乙基)-3,5-二苯基-1H-吡唑及其4-溴衍生物的对甲苯磺酸酯反应合成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)。一些化合物(V)在小鼠中表现出显著的镇痛活性。此外，上述化合物在大鼠中通常表现出适度的降压、减慢心率和抗炎活性，在小鼠中表现出浸润麻醉作用，以及在体外具有较弱的血小板抗聚集活性。

相似文献

1
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.3,5-二苯基-1H-吡唑衍生物。II-N-取代的1-(2-氨基乙基)-3,5-二苯基-1H-吡唑及其具有镇痛和其他活性的4-溴衍生物。
Farmaco Sci. 1988 Dec;43(12):1019-34.
2
3,5-Diphenyl-1H-pyrazole derivatives. III--Esters from 1-(2-hydroxyethyl)-3,5-diphenyl-1H-pyrazole and its 4-bromo derivative with hypotensive, depressant, antiarrhythmic and analgesic activities.
Farmaco. 1989 Jul-Aug;44(7-8):655-70.
3
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.
Farmaco Sci. 1988 Sep;43(9):725-43.
4
3,5-Diphenyl-1H-pyrazole derivatives. X. N-substituted 1-(2-aminopropyl)- and 1-(3-amino-2-hydroxypropyl)-3,5-diphenyl-1H-pyrazoles with antiinflammatory and other activities.3,5-二苯基-1H-吡唑衍生物。X. 具有抗炎及其他活性的N-取代的1-(2-氨基丙基)-和1-(3-氨基-2-羟丙基)-3,5-二苯基-1H-吡唑
Farmaco. 1992 Oct;47(10):1235-48.
5
3,5-Diphenyl-1H-pyrazole derivatives. V--1-Acetyl-4-hydroxy-3,5-diphenyl-2-pyrazoline esters, 4-hydroxy-3,5-diphenyl-1H-pyrazole esters and N-substituted 4-(3-amino-2-hydroxy-1-propoxy)-1-methyl-3,5-diphenyl-1H-pyrazoles with antiarrhythmic, sedative and platelet antiaggregating activities.3,5-二苯基-1H-吡唑衍生物。V——具有抗心律失常、镇静和血小板抗聚集活性的1-乙酰基-4-羟基-3,5-二苯基-2-吡唑啉酯、4-羟基-3,5-二苯基-1H-吡唑酯以及N-取代的4-(3-氨基-2-羟基-1-丙氧基)-1-甲基-3,5-二苯基-1H-吡唑
Farmaco. 1990 Feb;45(2):147-66.
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3,5-Diphenyl-1H-pyrazole derivatives. XII. N-substituted 4-amino-1-(2-hydroxy- or 2-alkylaminoethyl)-3,5-diphenyl-1H-pyrazoles with local anesthetic, analgesic and platelet antiaggregating activities.
Farmaco. 1994 Sep;49(9):533-40.
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3,5-Diphenyl-1H-pyrazole derivatives. VI--Esters and 2-dialkylaminoethyl ethers of 1(2-hydroxy-2-phenylethyl)-3,5-diphenyl-1H-pyrazole and N,N-disubstituted 1-(2-amino-2-phenylethyl)-3,5-diphenyl-1H-pyrazoles with depressant and platelet antiaggregating activities.3,5-二苯基-1H-吡唑衍生物。VI——1-(2-羟基-2-苯乙基)-3,5-二苯基-1H-吡唑的酯类和2-二烷基氨基乙基醚类以及具有镇静和血小板抗聚集活性的N,N-二取代-1-(2-氨基-2-苯乙基)-3,5-二苯基-1H-吡唑
Farmaco. 1990 May;45(5):511-26.
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3,5-Diphenyl-1H-pyrazole derivatives. IV--N,N-disubstituted 3-(3,5-diphenyl-1H-pyrazol-1-yl)propanamides and 3-(3,5-diphenyl-1H-pyrazol-1-yl)propanamines with sedative, platelet antiaggregating and local anesthetic activities.3,5-二苯基-1H-吡唑衍生物。IV——具有镇静、抗血小板聚集和局部麻醉活性的N,N-二取代3-(3,5-二苯基-1H-吡唑-1-基)丙酰胺和3-(3,5-二苯基-1H-吡唑-1-基)丙胺
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3,5-diphenyl-1H-pyrazole derivatives. XI. N-aryl-5(3)-phenyl-4-(3,5- diphenyl-1-pyrazolyl)-3(5)-pyrazole amines, 5-substituted 4,5-dihydro-3-phenyl-4-(3,5-diphenyl-1-pyrazolyl)-1H-pyrazoles and 2,6-disubstituted 1,6-dihydro-4- phenyl-5-(3,5-diphenyl-1-pyrazolyl)pyrimidines with antipyretic, antiinflammatory and other activities.3,5-二苯基-1H-吡唑衍生物。XI. N-芳基-5(3)-苯基-4-(3,5-二苯基-1-吡唑基)-3(5)-吡唑胺、5-取代的4,5-二氢-3-苯基-4-(3,5-二苯基-1-吡唑基)-1H-吡唑以及具有解热、抗炎和其他活性的2,6-二取代-1,6-二氢-4-苯基-5-(3,5-二苯基-1-吡唑基)嘧啶
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3,5-Diphenyl-1H-pyrazole derivatives. VII--Esters, 2-dialkylaminoethyl ethers and N-substituted carbamates of 1-(2-hydroxy-3-phenoxypropyl)-3,5-diphenyl-1H-pyrazole with depressant and platelet antiaggregating activities.
Farmaco. 1990 May;45(5):527-43.

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