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Design, synthesis, and PPARalpha/gamma agonistic activity of novel tetrahydroisoquinoline derivatives / 药学学报
Acta Pharmaceutica Sinica ; (12): 311-316, 2011.
Artigo em Chinês | WPRIM | ID: wpr-348959
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.
Assuntos
Texto completo: DisponíveL Índice: WPRIM (Pacífico Ocidental) Assunto principal: Farmacologia / Relação Estrutura-Atividade / Transfecção / Desenho de Fármacos / Química / Tetra-Hidroisoquinolinas / PPAR alfa / PPAR gama / Células HEK293 / Hipoglicemiantes Limite: Humanos Idioma: Chinês Revista: Acta Pharmaceutica Sinica Ano de publicação: 2011 Tipo de documento: Artigo

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Texto completo: DisponíveL Índice: WPRIM (Pacífico Ocidental) Assunto principal: Farmacologia / Relação Estrutura-Atividade / Transfecção / Desenho de Fármacos / Química / Tetra-Hidroisoquinolinas / PPAR alfa / PPAR gama / Células HEK293 / Hipoglicemiantes Limite: Humanos Idioma: Chinês Revista: Acta Pharmaceutica Sinica Ano de publicação: 2011 Tipo de documento: Artigo