| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 10588868 | Bioorganic & Medicinal Chemistry Letters | 2010 | 5 Pages |
Abstract
Here we report the discovery and early SAR of a series of mGluR5 negative allosteric modulators (NAMs). Starting from a moderately active HTS hit we synthesized 3,5-disubstituted-oxadiazoles and tetrazoles as mGluR5 NAMs. Based on the analysis of ligand efficiency and lipophilic efficiency metrics we identified a promising lead candidate as a starting point for further optimization.
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Authors
Gábor Wágner, Csaba Wéber, Olga Nyéki, Katalin Nógrádi, Attila Bielik, László Molnár, Amrita Bobok, Attila Horváth, Béla Kiss, Sándor Kolok, József Nagy, Dalma Kurkó, Krisztina Gál, István Greiner, Zsolt Szombathelyi, György M. Keserű,