Revista: | Quimica nova |
Base de datos: | PERIÓDICA |
Número de sistema: | 000199622 |
ISSN: | 0100-4042 |
Autors: | Barreiro, Eliezer J1 Fraga, Carlos A.M Miranda, Ana L.P Rodrigues, Carlos R |
Institucions: | 1Universidade Federal do Rio de Janeiro, Faculdade de Farmacia, Rio de Janeiro. Brasil |
Any: | 2002 |
Període: | Ene-Feb |
Volum: | 25 |
Número: | 1 |
Paginació: | 129-148 |
País: | Brasil |
Idioma: | Portugués |
Tipo de documento: | Artículo |
Enfoque: | Teórico, divulgación |
Resumen en inglés | 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 |
Disciplines | Química, Medicina |
Paraules clau: | Química farmacéutica, Química orgánica, Farmacología, Hidrazonas, Acilhidrazonas, Compuestos prototipo, Derivados, Analgésicos, Relación estructura-actividad, Diseño de fármacos |
Keyword: | Chemistry, Medicine, Medicinal chemistry, Organic chemistry, Pharmacology, Hydrazones, Acylhydrazones, Prototype compounds, Derivatives, Analgesics, Structure-activity relationship, Drug design |
Text complet: | Texto completo (Ver HTML) |