a química medicinal de n-acilidrazonas: novos compostos-protótipos de fármacos analgésicos, antiinflamatórios e anti-trombóticos medicinal chemistry of n-acylhydrazones: novel lead-compounds of analgesic, antiinflammatory and antithrombotic drugs
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a química medicinal de n-acilidrazonas: novos compostos-protótipos de fármacos analgésicos, antiinflamatórios e anti-trombóticos medicinal chemistry of n-acylhydrazones: novel lead-compounds of analgesic, antiinflammatory and antithrombotic drugs

;Eliezer J. Barreiro;Carlos A. M. Fraga;Ana L. P. Miranda;Carlos R. Rodrigues
greece and rome 2002 Vol. 25 pp. 129-148
237
barreiro2002qumicaa

Abstract

In this article are described new bioactive N-acylhydrazone (NAH) derivatives, structurally designed as optimization of aryl hydrazones precursors planned by molecular hybridization of two 5-lipoxigenase inhibitors, e.g. CBS-1108 and BW-755c. The analgesic, antiedematogenic and anti-platelet aggregating profile of several isosteric compounds was investigated by using classic pharmacological assays in vivo and ex-vivo, allowing to identify new potent peripheric analgesic lead, a new anti-inflammatory and an antithrombotic agent. During this study was discovered dozen of active NAH compounds clarifying the structure-activity relationship for this series of NAH derivatives, indicating the pharmacophore character of the N-acylhydrazone functionality.

Keywords

antiinflammatory

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DOI:
10.1590/S0100-40422002000100022
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http://www.scielo.br/scielo.php?script=sci_arttext...

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