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


Autoria(s): Barreiro,Eliezer J.; Fraga,Carlos A. M.; Miranda,Ana L. P.; Rodrigues,Carlos R.
Data(s)

01/02/2002

Resumo

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.

Formato

text/html

Identificador

http://www.scielo.br/scielo.php?script=sci_arttext&pid=S0100-40422002000100022

Idioma(s)

pt

Publicador

Sociedade Brasileira de Química

Fonte

Química Nova v.25 n.1 2002

Palavras-Chave #bioactive N-acylhydrazones derivatives #antiinflammatory, analgesic and antithrombotic properties #molecular hybridization and bioisosterism in drug design
Tipo

journal article