A química medicinal de N-acilidrazonas: novos compostos-protótipos de fármacos analgésicos, antiinflamatórios e anti-trombóticos

Química Nova

Eliezer J. Barreiro¹  Carlos A. M. Fraga¹  Ana L. P. Miranda¹  Carlos R. Rodrigues¹ 

[1] ,Universidade Federal do Rio de Janeiro Faculdade de Farmácia Rio de Janeiro RJ

关键词: bioactive N-acylhydrazones derivatives;    antiinflammatory;    analgesic and antithrombotic properties;    molecular hybridization and bioisosterism in drug design;   

DOI  :  10.1590/S0100-40422002000100022

来源: SciELO

【 摘 要 】

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.

【 授权许可】

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