Journal
QUIMICA NOVA
Volume 25, Issue 1, Pages 129-148Publisher
SOC BRASILEIRA QUIMICA
DOI: 10.1590/S0100-40422002000100022
Keywords
bioactive N-acythydrazones derivatives; antinflammatory; analgesic and antithrombotic properties; molecular hybridization and bioisosterism in drug; design
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In this article are described new bioactive N-acylhydrazone (NAH) derivatives, structurally designed as optimization or 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 compound, clarifying the structure-activity relationship for this series of NAH derivatives, indicating the pharmacophore character of the N-acylhydrazone functionality.
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