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Synthesis and analgesic-antiinflammatory activities of novel acylarylhydrazones with a 5-phenyl-4-R-3-pyrrolyl-acyl moiety

Murineddu, Gabriele and Loriga, Giovanni and Gavini, Elisabetta and Peana, Alessandra Tiziana and Mulè, Antonio Calogero and Pinna, Gérard Aimé (2001) Synthesis and analgesic-antiinflammatory activities of novel acylarylhydrazones with a 5-phenyl-4-R-3-pyrrolyl-acyl moiety. Archiv der Pharmazie, Vol. 334 (12), p. 393-398. eISSN 1521-4184. Article.

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DOI: 10.1002/1521-4184(200112)

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Abstract

A new series of arylidene 5-phenyl-4-R-pyrrole-3-carbohydrazides 1a—j were prepared and evaluated for their analgesic-antiinflammatory activities. All synthesized compounds showed a significant analgesic action in mice after intraperitoneal administration at a dose of 100 μM/kg. Two of these, 1b, (4'-methylbenzylidene)-5-phenyl-1H-pyrrole-3-carbohydrazide, and 1d, (4'-chlorobenzylidene)-5-phenyl-1H-pyrrole-3-carbohydrazide, were found to be more potent as antinociceptive agents respect to dipyrone and indometacin, used as reference drugs. Among compounds 1, only 1b showed a moderate antiinflammatory effect in rats while 1d proved to be a potent non antiinflammatory analgesic.

Item Type:Article
ID Code:8863
Status:Published
Refereed:Yes
Uncontrolled Keywords:3-Acylarylhydrazones, bioisosteric replacement, analgesic-antiinflammatory activities
Subjects:Area 03 - Scienze chimiche > CHIM/09 Farmaceutico tecnologico applicativo
Area 05 - Scienze biologiche > BIO/14 Farmacologia
Area 03 - Scienze chimiche > CHIM/08 Chimica farmaceutica
Divisions:001 Università di Sassari > 01 Dipartimenti > Farmaco, chimico, tossicologico
001 Università di Sassari > 01 Dipartimenti > Scienze del farmaco
Publisher:Wiley
eISSN:1521-4184
Copyright Holders:© WILEY-VCH Verlag GmbH, D-69451 Weinheim, 2001
Deposited On:11 Apr 2013 08:57

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