Synthesis and SAR of novel, 4-(phenylsulfamoyl)phenylacetamide mGlu4 positive allosteric modulators (PAMs) identified by functional high-throughput screening (HTS)
Research output: Contribution to journal › Journal article › Research › peer-review
Herein we disclose the synthesis and SAR of a series of 4-(phenylsulfamoyl)phenylacetamide compounds as mGlu(4) positive allosteric modulators (PAMs) that were identified via a functional HTS. An iterative parallel approach to these compounds culminated in the discovery of VU0364439 (11) which represents the most potent (19.8 nM) mGlu(4) PAM reported to date.
| Original language | English |
|---|---|
| Journal | Bioorganic & Medicinal Chemistry Letters |
| Volume | 20 |
| Issue number | 17 |
| Pages (from-to) | 5175-8 |
| Number of pages | 4 |
| ISSN | 0960-894X |
| DOIs | |
| Publication status | Published - 1 Sep 2010 |
| Externally published | Yes |
Bibliographical note
Copyright 2010 Elsevier Ltd. All rights reserved.
- Allosteric Regulation, Aniline Compounds/chemical synthesis, Receptors, Metabotropic Glutamate/drug effects, Structure-Activity Relationship, Sulfonamides/chemical synthesis
Research areas
ID: 213625970