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Future Med Chem ; 11(15): 1871-1882, 2019 08.
Artículo en Inglés | MEDLINE | ID: mdl-31517535

RESUMEN

Aim: Everyday studies prove the increasing need for newer and safer agents to control cellular inflammatory response, an underlying cause for the pathophysiology of many other clinical cases. Results: Two newly designed sets of schiff 5a-h and chlacone 6a-f substituted pyrazoles were synthesized and evaluated for their in vivo/vitro anti-inflammatory activities. Most potent representatives were chosen for investigation of ulcerogenic and molecular docking properties. Conclusion: The synthesized compounds showed considerable edema inhibition percentage range if compared with celecoxib (13-93% and 58-93%, respectively) at different time intervals. Compound 6e showed the best screening results if compared with celecoxib (inhibition % = 93.62 and 93.51% at 5 h, COX-1/COX-2 selectivity index SI = 215.44 and 308.16 and ulcer index = 7.25 and 8, respectively).


Asunto(s)
Antiinflamatorios/química , Ciclooxigenasa 1/química , Ciclooxigenasa 2/química , Pirazoles/química , Animales , Antiinflamatorios/metabolismo , Antiinflamatorios/uso terapéutico , Sitios de Unión , Dominio Catalítico , Celecoxib/farmacología , Celecoxib/uso terapéutico , Ciclooxigenasa 1/metabolismo , Ciclooxigenasa 2/metabolismo , Edema/inducido químicamente , Edema/tratamiento farmacológico , Edema/veterinaria , Enlace de Hidrógeno , Masculino , Simulación del Acoplamiento Molecular , Pirazoles/metabolismo , Ratas , Ratas Wistar , Relación Estructura-Actividad
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