Publications by authors named "Joseph D Panarese"

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Discovery of VU0467319: an M Positive Allosteric Modulator Candidate That Advanced into Clinical Trials.
Michael S Poslunsey, Michael R Wood, Changho Han, Shaun R Stauffer, Joseph D Panarese

ACS Chem Neurosci· January 2025

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High-Affinity Alkynyl Bisubstrate Inhibitors of Nicotinamide -Methyltransferase (NNMT).
Rocco L Policarpo, Ludovic Decultot, Elizabeth May, Petr Kuzmič, Samuel Carlson, Joseph D Panarese

J Med Chem· November 2019

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Discovery of VU2957 (Valiglurax): An mGlu Positive Allosteric Modulator Evaluated as a Preclinical Candidate for the Treatment of Parkinson's Disease.
Joseph D Panarese, Darren W Engers, Yong-Jin Wu, Joanne J Bronson, John E Macor

ACS Med Chem Lett· March 2019

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Discovery, Structure-Activity Relationship, and Biological Characterization of a Novel Series of 6-((1 H-Pyrazolo[4,3- b]pyridin-3-yl)amino)-benzo[ d]isothiazole-3-carboxamides as Positive Allosteric Modulators of the Metabotropic Glutamate Receptor 4 (mGlu).
Sean R Bollinger, Darren W Engers, Joseph D Panarese, Mary West, Julie L Engers

J Med Chem· January 2019

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The discovery of VU0652957 (VU2957, Valiglurax): SAR and DMPK challenges en route to an mGlu PAM development candidate.
Joseph D Panarese, Darren W Engers, Yong-Jin Wu, Jason M Guernon, Aspen Chun

Bioorg Med Chem Lett· January 2019

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Discovery and characterization of N-(1,3-dialkyl-1H-indazol-6-yl)-1H-pyrazolo[4,3-b]pyridin-3-amine scaffold as mGlu positive allosteric modulators that mitigate CYP1A2 induction liability.
Darren W Engers, Sean R Bollinger, Julie L Engers, Joseph D Panarese, Megan M Breiner

Bioorg Med Chem Lett· August 2018

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The discovery of VU0486846: steep SAR from a series of M PAMs based on a novel benzomorpholine core.
Jeanette L Bertron, Hyekyung P Cho, Pedro M Garcia-Barrantes, Joseph D Panarese, James M Salovich

Bioorg Med Chem Lett· July 2018

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Further optimization of the M1 PAM VU0453595: Discovery of novel heterobicyclic core motifs with improved CNS penetration.
Joseph D Panarese, Hykeyung P Cho, Jeffrey J Adams, Kellie D Nance, Pedro M Garcia-Barrantes

Bioorg Med Chem Lett· August 2016

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Discovery of 3-aminopicolinamides as metabotropic glutamate receptor subtype 4 (mGlu4) positive allosteric modulator warheads engendering CNS exposure and in vivo efficacy.
Rocco D Gogliotti, Darren W Engers, Pedro M Garcia-Barrantes, Joseph D Panarese, Patrick R Gentry

Bioorg Med Chem Lett· June 2016

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Discovery and SAR of muscarinic receptor subtype 1 (M1) allosteric activators from a molecular libraries high throughput screen. Part 1: 2,5-dibenzyl-2H-pyrazolo[4,3-c]quinolin-3(5H)-ones as positive allosteric modulators.
Changho Han, Arindam Chatterjee, Meredith J Noetzel, Joseph D Panarese, Emery Smith

Bioorg Med Chem Lett· January 2015

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Allosteric modulation of the M1 muscarinic acetylcholine receptor: improving cognition and a potential treatment for schizophrenia and Alzheimer's disease.
Bruce J Melancon, James C Tarr, Joseph D Panarese, Michael R Wood, Craig W Lindsley

Drug Discov Today· December 2013

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Tandem iodine-mediated oxidations of tetrahydro-β-carbolines: total synthesis of eudistomins Y1-Y7.
Joseph D Panarese, Stephen P Waters

Org Biomol Chem· June 2013

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Spiroaminal Model Systems of the Marineosins with Final Step Pyrrole Incorporation.
Joseph D Panarese, Leah C Konkol, Cynthia B Berry, Brittney S Bates, Leslie N Aldrich

Tetrahedron Lett· May 2013

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Biomimetic synthesis and biological evaluation of Aplidiopsamine A.
Joseph D Panarese, Craig W Lindsley

Org Lett· November 2012

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Room-temperature aromatization of tetrahydro-β-carbolines by 2-iodoxybenzoic acid: utility in a total synthesis of eudistomin U.
Joseph D Panarese, Stephen P Waters

Org Lett· September 2010

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Enantioselective formal total synthesis of (+)-aspergillide C.
Joseph D Panarese, Stephen P Waters

Org Lett· November 2009

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