Positive Allosteric Modulators for mGluR2 Receptors: A Medicinal Chemistry Perspective

Title:Positive Allosteric Modulators for mGluR2 Receptors: A Medicinal Chemistry Perspective

Volume: 14 Issue: 15

Author(s): Gyorgy Szabo and Gyorgy Miklos Keseru

Affiliation:

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

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.

Cite this article as:

Szabo Gyorgy and Keseru Miklos Gyorgy, Positive Allosteric Modulators for mGluR2 Receptors: A Medicinal Chemistry Perspective, Current Topics in Medicinal Chemistry 2014; 14 (15) . https://dx.doi.org/10.2174/1568026614666140826120716