Literature DB >> 19640716

Synthesis and SAR of a novel positive allosteric modulator (PAM) of the metabotropic glutamate receptor 4 (mGluR4).

Richard Williams1, Kari A Johnson, Patrick R Gentry, Colleen M Niswender, Charles D Weaver, P Jeffrey Conn, Craig W Lindsley, Corey R Hopkins.   

Abstract

This Letter describes the synthesis and SAR of the novel positive allosteric modulator, VU0155041, a compound that has shown in vivo efficacy in rodent models of Parkinson's disease. The synthesis takes advantage of an iterative parallel synthesis approach to rapidly synthesize and evaluate a number of analogs of VU0155041.

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Year:  2009        PMID： 19640716      PMCID： PMC2752865          DOI： 10.1016/j.bmcl.2009.07.072

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  17 in total

1.  Development of a custom high-throughput preparative liquid chromatography/mass spectrometer platform for the preparative purification and analytical analysis of compound libraries.

Authors:  William Leister; Kimberly Strauss; David Wisnoski; Zhijian Zhao; Craig Lindsley
Journal:  J Comb Chem       Date:  2003 May-Jun

2.  Synthesis and angiotensin II receptor antagonistic activities of benzimidazole derivatives bearing acidic heterocycles as novel tetrazole bioisosteres.

Authors:  Y Kohara; K Kubo; E Imamiya; T Wada; Y Inada; T Naka
Journal:  J Med Chem       Date:  1996-12-20       Impact factor: 7.446

3.  Allosteric modulation of group III metabotropic glutamate receptor 4: a potential approach to Parkinson's disease treatment.

Authors:  Michael J Marino; David L Williams; Julie A O'Brien; Ornella Valenti; Terrence P McDonald; Michelle K Clements; Ruiping Wang; Anthony G DiLella; J Fred Hess; Gene G Kinney; P Jeffrey Conn
Journal:  Proc Natl Acad Sci U S A       Date:  2003-10-30       Impact factor: 11.205

4.  Discovery, characterization, and antiparkinsonian effect of novel positive allosteric modulators of metabotropic glutamate receptor 4.

Authors:  Colleen M Niswender; Kari A Johnson; C David Weaver; Carrie K Jones; Zixiu Xiang; Qingwei Luo; Alice L Rodriguez; Joy E Marlo; Tomas de Paulis; Analisa D Thompson; Emily L Days; Tasha Nalywajko; Cheryl A Austin; Michael Baxter Williams; Jennifer E Ayala; Richard Williams; Craig W Lindsley; P Jeffrey Conn
Journal:  Mol Pharmacol       Date:  2008-07-29       Impact factor: 4.436

5.  Positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4). Part II: Challenges in hit-to-lead.

Authors:  Richard Williams; Colleen M Niswender; Qingwei Luo; Uyen Le; P Jeffrey Conn; Craig W Lindsley
Journal:  Bioorg Med Chem Lett       Date:  2008-12-25       Impact factor: 2.823

6.  Design and synthesis of potent beta-secretase (BACE1) inhibitors with P1' carboxylic acid bioisosteres.

Authors:  Tooru Kimura; Yoshio Hamada; Monika Stochaj; Hayato Ikari; Ayaka Nagamine; Hamdy Abdel-Rahman; Naoto Igawa; Koushi Hidaka; Jeffrey-Tri Nguyen; Kazuki Saito; Yoshio Hayashi; Yoshiaki Kiso
Journal:  Bioorg Med Chem Lett       Date:  2006-02-14       Impact factor: 2.823

7.  Positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4): Part I. Discovery of pyrazolo[3,4-d]pyrimidines as novel mGluR4 positive allosteric modulators.

Authors:  Colleen M Niswender; Evan P Lebois; Qingwei Luo; Kwangho Kim; Hubert Muchalski; Huiyong Yin; P Jeffrey Conn; Craig W Lindsley
Journal:  Bioorg Med Chem Lett       Date:  2008-08-29       Impact factor: 2.823

Review 8.  Subtype-selective allosteric modulators of muscarinic receptors for the treatment of CNS disorders.

Authors:  P Jeffrey Conn; Carrie K Jones; Craig W Lindsley
Journal:  Trends Pharmacol Sci       Date:  2009-02-07       Impact factor: 14.819

Review 9.  Allosteric modulators of GPCRs: a novel approach for the treatment of CNS disorders.

Authors:  P Jeffrey Conn; Arthur Christopoulos; Craig W Lindsley
Journal:  Nat Rev Drug Discov       Date:  2009-01       Impact factor: 84.694

10.  Synthesis and biological evaluation of 1-amino-2-phosphonomethylcyclopropanecarboxylic acids, new group III metabotropic glutamate receptor agonists.

Authors:  Pauline Sibille; Sébastien Lopez; Isabelle Brabet; Ornella Valenti; Nadia Oueslati; Florence Gaven; Cyril Goudet; Hugues-Olivier Bertrand; Jacques Neyton; Michael J Marino; Marianne Amalric; Jean-Philippe Pin; Francine C Acher
Journal:  J Med Chem       Date:  2007-06-28       Impact factor: 7.446
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  11 in total

Review 1.  Comprehensive survey of chemical libraries for drug discovery and chemical biology: 2009.

Authors:  Roland E Dolle; Bertrand Le Bourdonnec; Karin Worm; Guillermo A Morales; Craig J Thomas; Wei Zhang
Journal:  J Comb Chem       Date:  2010-10-05

2.  Allosteric modulation of seven transmembrane spanning receptors: theory, practice, and opportunities for central nervous system drug discovery.

Authors:  Bruce J Melancon; Corey R Hopkins; Michael R Wood; Kyle A Emmitte; Colleen M Niswender; Arthur Christopoulos; P Jeffrey Conn; Craig W Lindsley
Journal:  J Med Chem       Date:  2012-01-06       Impact factor: 7.446

Review 3.  Recent progress on the identification of metabotropic glutamate 4 receptor ligands and their potential utility as CNS therapeutics.

Authors:  Albert J Robichaud; Darren W Engers; Craig W Lindsley; Corey R Hopkins
Journal:  ACS Chem Neurosci       Date:  2011-06-14       Impact factor: 4.418

4.  Discovery of N-(4-methoxy-7-methylbenzo[d]thiazol-2-yl)isonicatinamide, ML293, as a novel, selective and brain penetrant positive allosteric modulator of the muscarinic 4 (M4) receptor.

Authors:  James M Salovich; Paige N Vinson; Douglas J Sheffler; Atin Lamsal; Thomas J Utley; Anna L Blobaum; Thomas M Bridges; Uyen Le; Carrie K Jones; Michael R Wood; J Scott Daniels; P Jeffrey Conn; Colleen M Niswender; Craig W Lindsley; Corey R Hopkins
Journal:  Bioorg Med Chem Lett       Date:  2012-06-06       Impact factor: 2.823

5.  Putative mGluR4 positive allosteric modulators activate Gi-independent anti-inflammatory mechanisms in microglia.

Authors:  Gelareh Abulwerdi; Bogdan A Stoica; David J Loane; Alan I Faden
Journal:  Neurochem Int       Date:  2020-05-23       Impact factor: 3.921

6.  Solution-phase parallel synthesis and SAR of homopiperazinyl analogs as positive allosteric modulators of mGlu₄.

Authors:  Yiu-Yin Cheung; Rocio Zamorano; Anna L Blobaum; C David Weaver; P Jeffrey Conn; Craig W Lindsley; Colleen M Niswender; Corey R Hopkins
Journal:  ACS Comb Sci       Date:  2011-02-21       Impact factor: 3.784

7.  Synthesis and SAR of novel, 4-(phenylsulfamoyl)phenylacetamide mGlu4 positive allosteric modulators (PAMs) identified by functional high-throughput screening (HTS).

Authors:  Darren W Engers; Patrick R Gentry; Richard Williams; Julie D Bolinger; C David Weaver; Usha N Menon; P Jeffrey Conn; Craig W Lindsley; Colleen M Niswender; Corey R Hopkins
Journal:  Bioorg Med Chem Lett       Date:  2010-07-08       Impact factor: 2.823

8.  Therapeutic potential of targeting metabotropic glutamate receptors for Parkinson's disease.

Authors:  Jonathan W Dickerson; P Jeffrey Conn
Journal:  Neurodegener Dis Manag       Date:  2012-04-01

9.  The functional cooperation of 5-HT1A and mGlu4R in HEK-293 cell line.

Authors:  Grzegorz Burnat; Piotr Brański; Joanna Solich; Magdalena Kolasa; Barbara Chruścicka; Marta Dziedzicka-Wasylewska; Andrzej Pilc
Journal:  Pharmacol Rep       Date:  2020-05-29       Impact factor: 3.024

10.  Challenges in the Discovery and Optimization of mGlu2/4 Heterodimer Positive Allosteric Modulators.

Authors:  Mark Gallant Fulton; Matthew Thomas Loch; Caroline Anne Cuoco; Alice Lambert Rodriguez; Emily Days; Paige Newton Vinson; Krystian Andrezej Kozek; Charles David Weaver; Anna Louise Blobaum; Peter Jeffrey Conn; Colleen Marie Niswender; Craig William Lindsley
Journal:  Lett Drug Des Discov       Date:  2019-12       Impact factor: 1.150
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