Synthesis of new chemical entities from paracetamol and NSAIDs with improved pharmacodynamic profile.
Bioorg Med Chem
; 14(24): 8701-6, 2006 Dec 15.
Article
en En
| MEDLINE
| ID: mdl-16962330
It was envisaged to combine high antipyretic activity of paracetamol into commonly used NSAIDs. To achieve this goal new chemical entities were synthesized by chemically combining paracetamol and NSAIDs, and biologically evaluated for their antipyretic, analgesic, anti-inflammatory and ulcerogenic potential. The acid chloride of parent NSAIDs was reacted with excess of p-aminophenol to yield the desired p-amidophenol derivatives (1B-7B). Acetate derivatives (1C-7C) of these phenols (1B-7B) were also prepared by their treatment with acetic anhydride, in order to see the impact of blocking the free phenolic group on the biological activity of the derivatives. All the synthesized p-amidophenol derivatives showed improved antipyretic activity than paracetamol with retention of anti-inflammatory activity of their parent NSAIDs. These compounds elicited no ulcerogenicity unlike their parent drugs.
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Colección:
01-internacional
Base de datos:
MEDLINE
Asunto principal:
Fenoles
/
Antiinflamatorios no Esteroideos
/
Inhibidores de la Ciclooxigenasa 2
/
Analgésicos
/
Acetaminofén
/
Antiinflamatorios
Límite:
Animals
Idioma:
En
Revista:
Bioorg Med Chem
Asunto de la revista:
BIOQUIMICA
/
QUIMICA
Año:
2006
Tipo del documento:
Article
País de afiliación:
India
Pais de publicación:
Reino Unido