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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.

作者信息

Bondavalli F, Bruno O, Ranise A, Schenone P, Addonizio P, De Novellis V, Loffreda A, Marmo E

机构信息

Istituto di Scienze Farmaceutiche, Università di Genova, Italy.

出版信息

Farmaco Sci. 1988 Sep;43(9):725-43.

PMID:3229497
Abstract

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.

摘要

相似文献

1
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.
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. 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.
4
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.
5
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.
6
3,5-Diphenyl-1H-pyrazole derivatives. VIII. N-substituted 3-(4-hydroxy-3,5-diphenyl-1H-pyrazol-1-yl)-propanamides, -propanamines and 2-(4-hydroxy-3,5-diphenyl-1H-pyrazol-1-yl)ethanamines with platelet antiaggregating, hypotensive, antiarrhythmic and other activities.3,5-二苯基-1H-吡唑衍生物。VIII. N-取代的3-(4-羟基-3,5-二苯基-1H-吡唑-1-基)丙酰胺、丙胺及2-(4-羟基-3,5-二苯基-1H-吡唑-1-基)乙胺,具有抗血小板聚集、降压、抗心律失常及其他活性。
Farmaco. 1991 Mar;46(3):477-99.
7
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.
8
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.
9
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.
10
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
Farmaco. 1990 Feb;45(2):137-46.

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