Novel unsaturated glycyrrhetic acids derivatives: Design, synthesis and anti-inflammatory activity.
Eur J Med Chem
; 139: 337-348, 2017 Oct 20.
Article
en En
| MEDLINE
| ID: mdl-28803048
ABSTRACT
To develop novel anti-inflammatory agents, a series of unsaturated glycyrrhetic acids were designed, synthesized and evaluated for anti-inflammatory activity using RAW264.7 cells. The structure-activity relationship (SAR) of NO inhibitory activity was analyzed. α,ß-Unsaturated glycyrrhetic acids showed better activity, among them, compounds 6k and 6l with piperazine unit exhibited the most potent nitric oxide (NO) and interleukin-6 (IL-6) inhibitory activity (IC50 = 13.3 and 15.5 µM respectively). Furthermore, compound 6k could also significantly suppress LPS-induced iNOS and COX-2 expression and IL-6 production through MAPKs and NF-kB signaling pathway.
Palabras clave
Texto completo:
1
Base de datos:
MEDLINE
Asunto principal:
Diseño de Fármacos
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Antiinflamatorios no Esteroideos
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Interleucina-6
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Ácido Glicirretínico
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Óxido Nítrico
Tipo de estudio:
Prognostic_studies
Idioma:
En
Revista:
Eur J Med Chem
Año:
2017
Tipo del documento:
Article