Design, synthesis, and PPARalpha/gamma agonistic activity of novel tetrahydroisoquinoline derivatives / 药学学报
Acta Pharmaceutica Sinica
; (12): 311-316, 2011.
Article
em Zh
| WPRIM
| ID: wpr-348959
Biblioteca responsável:
WPRO
ABSTRACT
A series of tetrahydroisoquinoline derivatives were prepared and their peroxisome proliferator-activated receptor (PPAR) alpha/gamma agonistic activities were evaluated to obtain more potent PPAR agonist. All of them were new compounds, and their structures were confirmed by 1H NMR and HR-MS. Three compounds exhibited higher agonistic activities of PPARgamma than that of the comparison, six compounds exhibited higher agonistic activities of PPARalpha than that of the comparison, and compound 8a was discovered as a highly potent PPARalpha/gamma agonist that is much more active than that of WY14643 and rosiglitazone. The development of potent PPAR agonists may offer a new choice for the treatment of diabetes.
Texto completo:
1
Índice:
WPRIM
Assunto principal:
Farmacologia
/
Relação Estrutura-Atividade
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Transfecção
/
Desenho de Fármacos
/
Química
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Tetra-Hidroisoquinolinas
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PPAR alfa
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PPAR gama
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Células HEK293
/
Hipoglicemiantes
Limite:
Humans
Idioma:
Zh
Revista:
Acta Pharmaceutica Sinica
Ano de publicação:
2011
Tipo de documento:
Article