Design and synthesis of 3,4-methylenedioxy-6-nitrophenoxyacetylhydrazone derivatives obtained from natural safrole: new lead-agents with analgesic and antipyretic properties.
Bioorg Med Chem
; 14(23): 7924-35, 2006 Dec 01.
Article
en En
| MEDLINE
| ID: mdl-16904329
In this work, we reported the synthesis and evaluation of the analgesic, anti-inflammatory, and antipyretic properties of new 2-(6-nitro-benzo[1,3]dioxol-5-yloxy)-acetylhydrazone derivatives (3), designed exploring molecular hybridization and isosteric replacement approaches between nimesulide (1) and carbanalogue NAH series (2) developed at LASSBio. Target compounds were synthesized in very good yields exploiting abundant Brazilian natural product safrole (4) as starting material. The evaluation of the antinociceptive properties of this series led us to discover a new potent prototype of analgesic and antipyretic agent, that is, NAH derivative 3c, named LASSBio-891, which showed to be more potent than dipyrone used as standard.
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Bases de datos:
MEDLINE
Asunto principal:
Safrol
/
Analgésicos no Narcóticos
/
Hidrazonas
/
Analgésicos
Idioma:
En
Revista:
Bioorg Med Chem
Año:
2006
Tipo del documento:
Article
País de afiliación:
Brasil