Positive Allosteric Modulators for mGluR2 Receptors: A Medicinal Chemistry Perspective

Author(s): Gyorgy Szabo, Gyorgy Miklos Keseru

Journal Name: Current Topics in Medicinal Chemistry

Volume 14 , Issue 15 , 2014

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Graphical Abstract:


This review summarizes drug discovery efforts on mGluR2 positive allosteric modulators (PAMs) from 2000 to 2013. Medicinal chemistry programs and the identified 21 chemotypes are analyzed and compared in terms of their biological activity and ligand efficiency. Comparative analysis of ligand efficiency metrics including ligand efficiency and lipophilic ligand efficiency allowed us to identify the most promising chemotypes. The perspective of their clinical development was evaluated in the light of recent human data.

Keywords: Clinical development, ligand efficiency, medicinal chemistry, mGluR2 receptors, positive allosteric modulators.

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Article Details

Year: 2014
Published on: 28 September, 2014
Page: [1771 - 1788]
Pages: 18
DOI: 10.2174/1568026614666140826120716
Price: $65

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PDF: 46