An Overview of Recent Dipeptidyl Peptidase-IV Inhibitors: Linking their Structure and Physico-Chemical Properties with SAR, Pharmacokinetics and Toxicity

Author(s): Andrija Smelcerovic, Filip Miljkovic, Ana Kolarevic, Jelena Lazarevic, Aleksandra Djordjevic, Gordana Kocic, Marko Anderluh

Journal Name: Current Topics in Medicinal Chemistry

Volume 15 , Issue 23 , 2015

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Graphical Abstract:


Dipeptidyl peptidase-IV (DPP-IV) (EC is а member of the broad class of hydrolytic enzymes which is responsible for degradation of the incretin peptide hormones regulating blood glucose levels. In this article we review the literature on natural and synthetic DPP-IV inhibitors, focusing their chemical structure and mechanism of action. Further, physico-chemical, pharmacokinetic and toxicological properties of DPP-IV inhibitors are calculated and compared. On the basis of literature data we selected the DPP-IV inhibitors with IC50 values below 1 nM and discussed their possible application in therapy of type 2 diabetes mellitus.

Keywords: Dipeptidyl peptidase-IV inhibitors, Pharmacokinetic properties, Physico-chemical properties, SAR, Toxicological properties, Type 2 diabetes mellitus.

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Article Details

Year: 2015
Published on: 20 August, 2015
Page: [2342 - 2372]
Pages: 31
DOI: 10.2174/1568026615666150619142731
Price: $65

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PDF: 41