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SYNTHESIS OF NEW 3-PHENYLPROPIONIC ACID DERIVATIVES HAVING ANTIDIABETIC ACTIVITY

Zbigniew Majka ,  Katarzyna Rusin ,  Dominik Kłudkiewicz ,  Andrzej W. Sawicki ,  Tomasz Stawiński ,  Anna Lendzion 

Adamed, Czosnów, Pieńków 05-152, Poland

Abstract

Diseases such as hyperlipidemia, atherosclerosis, obesity, and type 2 diabetes become the serious concern not only for developed industrial societies. It is estimated that more than 150 million people worldwide suffer from type 2 diabetes, and this number is expected to double by 2025. In Poland, currently about 2 million people suffer from this disease, and the same number is at risk of developing it. Costs of medical care in diabetic patients reach 6 to 8 percent of total medical care budgets.

More than 20 years ago, the thiazolidinedione group of compounds was discovered, showing the activity in rodent models of type 2 diabetes and insulin resistance. Although their mechanism of action was not known, the compounds have been successfully used in therapy of type 2 diabetes. Publications demonstrating that they exerted their effect via the nuclear PPAR gamma receptor were published only in the middle of 90's. Now, it is well known that intracellular receptor proteins of the PPAR family control the expression of genes involved in the regulation of lipid-carbohydrate metabolism.

We synthetised three groups of compounds with antidiabetic activity. Experiments showed the high affinity of obtained compounds to PPARg receptor.

 

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Related papers

Presentation: Poster at V Multidyscyplinarna Konferencja Nauki o Leku, by Zbigniew Majka
See On-line Journal of V Multidyscyplinarna Konferencja Nauki o Leku

Submitted: 2006-03-23 14:01
Revised:   2009-06-07 00:44