RESUMEN

We have designed and synthesized a series of novel molecules having a residue of a classical NSAID and an antioxidant moiety, both attached through amide bonds to a known nootropic structure, an L-proline, trans-4-hydroxy-L-proline or DL-pipecolinic acid residue. The compounds were found to retain anti-inflammatory and antioxidant activities, to acquire hypocholesterolemic action, and to possess a greatly reduced gastrointestinal toxicity. The novel molecules could find useful applications, among others, in slowing the progression or delaying the onset of neurodegenerative diseases.

Asunto(s)

Antiinflamatorios no Esteroideos/farmacología , Antioxidantes/farmacología , Artritis/tratamiento farmacológico , Inflamación/tratamiento farmacológico , Ácidos Pipecólicos/farmacología , Prolina/farmacología , Animales , Antiinflamatorios no Esteroideos/síntesis química , Antiinflamatorios no Esteroideos/química , Anticolesterolemiantes/síntesis química , Anticolesterolemiantes/química , Anticolesterolemiantes/farmacología , Antioxidantes/síntesis química , Antioxidantes/química , Colesterol/sangre , Modelos Animales de Enfermedad , Diseño de Fármacos , Evaluación Preclínica de Medicamentos , Femenino , Ácidos Pipecólicos/síntesis química , Ácidos Pipecólicos/química , Prolina/análogos & derivados , Prolina/síntesis química , Ratas , Ratas Endogámicas F344 , Relación Estructura-Actividad , Triglicéridos/sangre