Discovery of biological evaluation of pyrazole/imidazole amides as mGlu5 receptor negative allosteric modulators

  • Bioorg Med Chem Lett. 2013 Apr 1;23(7):2134-9. doi: 10.1016/j.bmcl.2013.01.116.
Eunhee Chae  1 ,  Yong-Je Shin ,  Eun-Ju Ryu ,  Mi Kyung Ji ,  Nahm Ryune Cho ,  Ki-Ho Lee ,  Hyun Ji Jeong ,  Soo-Jin Kim ,  Yeonjung Choi ,  Kyung Seok Oh ,  Chun-Eung Park ,  Young Soo Yoon
Affiliations
  • 1. CNS Drug Discovery, Drug Development Center, SK Biopharmaceuticals, Daejeon 305-712, Republic of Korea. [email protected]
PMID: 23434029 DOI: 10.1016/j.bmcl.2013.01.116
Abstract

Development of SAR in a 5-aryl-3-acylpyridinyl-pyrazoles and 1-aryl-4-acylpyridinyl imidazoles series of mGlu5 receptor negative allosteric modulators (mGluR5 NAMs) using a functional cell-based assay is described in this Letter. Analysis of the Ligand-lipophilic efficiency (LipE) of compounds provided new insight for the design of potent mGluR5 negative allosteric modulators with anti-depressant activities.