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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.

作者信息

Bruno O, Ranise A, Bondavalli F, Schenone S, D'Amico M, Falciani M, Vacca C, Filippelli A

机构信息

Istituto di Scienze Farmaceutiche dell'Università, Genova, Italy.

出版信息

Farmaco. 1994 Sep;49(9):533-40.

PMID:7811347
Abstract

The synthesis of 4-amino-3,5-diphenyl-1H-pyrazole-1-ethanol, as well as of their N-methyl, N-ethyl and N,N-dimethyl derivatives is described. A series of 1-(2-alkylaminoethyl)-3,5-diphenyl-1H-pyrazole-4-amines and of N-substituted 4-dimethylamino-3,5-diphenyl-1H-pyrazole-1-ethanamines were also prepared. Some of the above compounds showed remarkable local anesthetic, analgesic and in vitro platelet antiaggregating activities, as well as moderate antiinflammatory and antipyretic activities in rats and mice.

摘要

相似文献

1
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.
2
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.
3
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.
4
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.
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. 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.
7
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
Farmaco. 1993 Jul;48(7):949-66.
8
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.
9
3,5-Diphenyl-1H-pyrazole derivatives. IX. 2-substituted 4-phenyl-5-(3,5-diphenyl-1H-pyrazol-1-yl) pyrimidines with platelet antiaggregating and other activities.3,5-二苯基-1H-吡唑衍生物。IX。具有血小板抗聚集及其他活性的2-取代-4-苯基-5-(3,5-二苯基-1H-吡唑-1-基)嘧啶
Farmaco. 1992 Feb;47(2):171-90.
10
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.