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[Synthesis of phenyloxyisobutyric acid derivatives and their antidiabetic activity in vitro].
Zeng, Qing-le; Wang, He-qing; Luo, Huan; Gao, Xiao-ping; Liu, Zhong-rong; Li, Bo-gang; Wang, Feng-peng; Zhao, Yu-fen.
Afiliação
  • Zeng QL; Department of Chemistry and Key Laboratory for Chemical Biology of Fujian Province, Xiamen University, Xiamen 361005, China. qlzeng@xmu.edu.cn
Yao Xue Xue Bao ; 41(2): 108-14, 2006 Feb.
Article em Zh | MEDLINE | ID: mdl-16671538
AIM: To design and synthesize new phenyloxyisobutyric acid analogues as antidiabetic compounds. METHODS: Eight new target compounds were synthesized by combination of lipophilic moieties and acidic moiety with nucleophilic replacement or Mitsunobu condensation. The eight compounds were confirmed by 1H NMR, 13C NMR, IR and MS. RESULTS: In vitro insulin-sensitizing activity (3T3-L1 adipocyte) demonstrated, that the cultured glucose concentration of up-clear solution detected with GOD-POD assay were 5.942, 6.339, 6.226 and 6.512 mmol x L(-1), respectively, when rosiglitazone, pioglitazone, compounds A and B were added to the insulin-resistant system. CONCLUSION: In vitro insulin-sensitizing activity of target compound A is in between that of rosiglitazone and pioglitazone, and activity of target compound B is slightly less than that of pioglitazone.
Assuntos
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Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Butiratos / PPAR gama / Hipoglicemiantes Limite: Animals Idioma: Zh Ano de publicação: 2006 Tipo de documento: Article
Buscar no Google
Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Butiratos / PPAR gama / Hipoglicemiantes Limite: Animals Idioma: Zh Ano de publicação: 2006 Tipo de documento: Article