title: Solution-phase parallel synthesis and SAR of homopiperazinyl analogs as positive allosteric modulators of mGlu₄.
abstract: Using a functional high-throughput screening (HTS) and subsequent solution-phase parallel synthesis approach, we have discovered a novel series of positive allosteric modulators for mGlu₄, a G-protein coupled receptor. This series is comprised of a homopiperazine central core. The solution-phase parallel synthesis and SAR of analogs derived from this series will be presented. This series of positive allosteric modulators of mGlu₄ provide critical research tools to further probe the mGlu₄-mediated effects in Parkinson's disease.
authors.affiliation: Department of Pharmacology, Vanderbilt Program in Drug Discovery, Vanderbilt University Medical Center, Nashville, TN 37232, United States.
authors.forename: Yiu-Yin
authors.initials: YY
authors.lastname: Cheung
authors.forename: Rocio
authors.initials: R
authors.lastname: Zamorano
authors.forename: Anna L
authors.initials: AL
authors.lastname: Blobaum
authors.forename: C David
authors.initials: CD
authors.lastname: Weaver
authors.forename: P Jeffrey
authors.initials: PJ
authors.lastname: Conn
authors.forename: Craig W
authors.initials: CW
authors.lastname: Lindsley
authors.forename: Colleen M
authors.initials: CM
authors.lastname: Niswender
authors.forename: Corey R
authors.initials: CR
authors.lastname: Hopkins
mesh_terms: D000494:Allosteric Regulation; D006801:Humans; D015394:Molecular Structure; D010879:Piperazines / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology; D018094:Receptors, Metabotropic Glutamate / Q000737:chemistry* / Q000187:drug effects; D013329:Structure-Activity Relationship
chemical_list: D010879:Piperazines; D018094:Receptors, Metabotropic Glutamate