Synthesis of phenyloxyisobutyric acid derivatives and their antidiabetic activity in vitro.
- Author:
Qing-le ZENG
1
;
He-qing WANG
;
Huan LUO
;
Xiao-ping GAO
;
Zhong-rong LIU
;
Bo-gang LI
;
Feng-peng WANG
;
Yu-fen ZHAO
Author Information
- Publication Type:Journal Article
- MeSH: 3T3-L1 Cells; Adipocytes; drug effects; Animals; Butyrates; chemical synthesis; chemistry; pharmacology; Hypoglycemic Agents; chemical synthesis; chemistry; pharmacology; Insulin; pharmacology; Mice; Molecular Structure; PPAR gamma; agonists; pharmacology
- From: Acta Pharmaceutica Sinica 2006;41(2):108-114
- CountryChina
- Language:Chinese
-
Abstract:
AIMTo design and synthesize new phenyloxyisobutyric acid analogues as antidiabetic compounds.
METHODSEight 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.
RESULTSIn 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.
CONCLUSIONIn 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.
