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Discovery of novel urea derivatives as dual-target hypoglycemic agents that activate glucokinase and PPARγ.
- Source :
-
European Journal of Medicinal Chemistry . Apr2014, Vol. 76, p182-192. 11p. - Publication Year :
- 2014
-
Abstract
- Abstract: Motivated by the discovery of a potential ligand that activates both glucokinase (GK) and perioxisome proliferator-activated receptor-γ (PPARγ), this work presents the rational design and synthesis of a series of novel urea derivatives as potent dual-target ligands of GK and PPARγ. The derivatives obtained, particularly compounds 14j, 14m, 15g, 15j, and 15s, showed relatively high enzyme activity and moderate blood glucose-lowering efficacy in normal ICR mice (GK activation fold >1.7, PPARγ activation percentage >38.8%, relative to rosiglitazone). The discovery of a dual-acting agent may provide an effective approach for treating type 2 diabetes mellitus. [Copyright &y& Elsevier]
Details
- Language :
- English
- ISSN :
- 02235234
- Volume :
- 76
- Database :
- Academic Search Index
- Journal :
- European Journal of Medicinal Chemistry
- Publication Type :
- Academic Journal
- Accession number :
- 95018209
- Full Text :
- https://doi.org/10.1016/j.ejmech.2014.02.024