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具有抗炎、镇痛、解热和血小板抗聚集活性的N-取代-4-羧基-1-苯基-1H-吡唑-5-丙酰胺

N-substituted 4-carboxy-1-phenyl-1H-pyrazole-5-propanamides with antiinflammatory, analgesic, antipyretic and platelet antiaggregating activities.

作者信息

Menozzi G, Mosti L, Schenone P, D'Amico M, Falzarano C, Rossi F

机构信息

Istituto di Scienze Farmaceutiche dell'Università Viale Benedetto XV, Genova, Italy.

出版信息

Farmaco. 1993 Apr;48(4):539-49.

PMID:8357469
Abstract

The synthesis of a series of N-substituted 4-carboxy-1-phenyl-1H-pyrazole-5-propanamides by reaction of 1-phenyl-1H-oxepino[4,3-c]pyrazole-4(8H),6(7H)-dione with aromatic primary amines is described. Some amides showed a platelet antiaggregating activity in vitro superior or comparable to that of acetylsalicylic acid, as well as moderate antiinflammatory, analgesic and antipyretic activities in rats or mice.

摘要

描述了通过1-苯基-1H-氧杂环庚三烯并[4,3-c]吡唑-4(8H),6(7H)-二酮与芳香伯胺反应合成一系列N-取代的4-羧基-1-苯基-1H-吡唑-5-丙酰胺的方法。一些酰胺在体外表现出优于或相当于乙酰水杨酸的血小板抗聚集活性，以及在大鼠或小鼠体内具有适度的抗炎、镇痛和解热活性。

相似文献

1
N-substituted 4-carboxy-1-phenyl-1H-pyrazole-5-propanamides with antiinflammatory, analgesic, antipyretic and platelet antiaggregating activities.具有抗炎、镇痛、解热和血小板抗聚集活性的N-取代-4-羧基-1-苯基-1H-吡唑-5-丙酰胺
Farmaco. 1993 Apr;48(4):539-49.
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Farmaco. 1992 Oct;47(10):1235-48.
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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
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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。
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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
Farmaco. 1993 Jul;48(7):949-66.
8
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.
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1-Aryl-1H-pyrazole-5-acetic acids with antiinflammatory, analgesic and other activities.具有抗炎、止痛及其他活性的1-芳基-1H-吡唑-5-乙酸
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