Literature DB >> 19469556

Synthesis and evaluation of a series of heterobiarylamides that are centrally penetrant metabotropic glutamate receptor 4 (mGluR4) positive allosteric modulators (PAMs).

Darren W Engers1, Colleen M Niswender, C David Weaver, Satyawan Jadhav, Usha N Menon, Rocio Zamorano, P Jeffrey Conn, Craig W Lindsley, Corey R Hopkins.   

Abstract

We report the synthesis and evaluation of a series of heterobiaryl amides as positive allosteric modulators of mGluR4. Compounds 9b and 9c showed submicromolar potency at both human and rat mGluR4. In addition, both 9b and 9c were shown to be centrally penetrant in rats using nontoxic vehicles, a major advance for the mGluR4 field.

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Year:  2009        PMID： 19469556      PMCID： PMC2765192          DOI： 10.1021/jm9005065

Source DB:  PubMed          Journal:  J Med Chem        ISSN： 0022-2623            Impact factor:   7.446


  16 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.  Group III metabotropic glutamate receptor-mediated modulation of the striatopallidal synapse.

Authors:  Ornella Valenti; Michael J Marino; Marion Wittmann; Edward Lis; Anthony G DiLella; Gene G Kinney; P Jeffrey Conn
Journal:  J Neurosci       Date:  2003-08-06       Impact factor: 6.167

3.  Ligand efficiency: a useful metric for lead selection.

Authors:  Andrew L Hopkins; Colin R Groom; Alexander Alex
Journal:  Drug Discov Today       Date:  2004-05-15       Impact factor: 7.851

Review 4.  Glutamate-based therapeutic approaches: allosteric modulators of metabotropic glutamate receptors.

Authors:  Michael J Marino; P Jeffrey Conn
Journal:  Curr Opin Pharmacol       Date:  2005-12-20       Impact factor: 5.547

5.  Discovery of positive allosteric modulators for the metabotropic glutamate receptor subtype 5 from a series of N-(1,3-diphenyl-1H- pyrazol-5-yl)benzamides that potentiate receptor function in vivo.

Authors:  Craig W Lindsley; David D Wisnoski; William H Leister; Julie A O'brien; Wei Lemaire; David L Williams; Maryann Burno; Cyrille Sur; Gene G Kinney; Doug J Pettibone; Philip R Tiller; Sheri Smith; Mark E Duggan; George D Hartman; P Jeffrey Conn; Joel R Huff
Journal:  J Med Chem       Date:  2004-11-18       Impact factor: 7.446

6.  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

7.  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

8.  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

9.  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 10.  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
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  38 in total

1.  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

2.  Discovery, synthesis, and structure-activity relationship development of a series of N-4-(2,5-dioxopyrrolidin-1-yl)phenylpicolinamides (VU0400195, ML182): characterization of a novel positive allosteric modulator of the metabotropic glutamate receptor 4 (mGlu(4)) with oral efficacy in an antiparkinsonian animal model.

Authors:  Carrie K Jones; Darren W Engers; Analisa D Thompson; Julie R Field; Anna L Blobaum; Stacey R Lindsley; Ya Zhou; Rocco D Gogliotti; Satyawan Jadhav; Rocio Zamorano; Jim Bogenpohl; Yoland Smith; Ryan Morrison; J Scott Daniels; C David Weaver; P Jeffrey Conn; Craig W Lindsley; Colleen M Niswender; Corey R Hopkins
Journal:  J Med Chem       Date:  2011-10-19       Impact factor: 7.446

3.  Iterative experimental and virtual high-throughput screening identifies metabotropic glutamate receptor subtype 4 positive allosteric modulators.

Authors:  Ralf Mueller; Eric S Dawson; Colleen M Niswender; Mariusz Butkiewicz; Corey R Hopkins; C David Weaver; Craig W Lindsley; P Jeffrey Conn; Jens Meiler
Journal:  J Mol Model       Date:  2012-05-17       Impact factor: 1.810

4.  Discovery of VU2957 (Valiglurax): An mGlu4 Positive Allosteric Modulator Evaluated as a Preclinical Candidate for the Treatment of Parkinson's Disease.

Authors:  Joseph D Panarese; Darren W Engers; Yong-Jin Wu; Joanne J Bronson; John E Macor; Aspen Chun; Alice L Rodriguez; Andrew S Felts; Julie L Engers; Matthew T Loch; Kyle A Emmitte; Arlindo L Castelhano; Michael J Kates; Michael A Nader; Carrie K Jones; Anna L Blobaum; P Jeffrey Conn; Colleen M Niswender; Corey R Hopkins; Craig W Lindsley
Journal:  ACS Med Chem Lett       Date:  2018-10-16       Impact factor: 4.345

Review 5.  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

6.  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

7.  The Concise Guide to PHARMACOLOGY 2013/14: G protein-coupled receptors.

Authors:  Stephen P H Alexander; Helen E Benson; Elena Faccenda; Adam J Pawson; Joanna L Sharman; Michael Spedding; John A Peters; Anthony J Harmar
Journal:  Br J Pharmacol       Date:  2013-12       Impact factor: 8.739

8.  Discovery and characterization of a novel series of N-phenylsulfonyl-1H-pyrrole picolinamides as positive allosteric modulators of the metabotropic glutamate receptor 4 (mGlu4).

Authors:  Rocco D Gogliotti; Anna L Blobaum; Ryan M Morrison; J Scott Daniels; James M Salovich; Yiu-Yin Cheung; Alice L Rodriguez; Matthew T Loch; P Jeffrey Conn; Craig W Lindsley; Colleen M Niswender; Corey R Hopkins
Journal:  Bioorg Med Chem Lett       Date:  2016-05-11       Impact factor: 2.823

Review 9.  Therapeutic potential of targeting group III metabotropic glutamate receptors in the treatment of Parkinson's disease.

Authors:  Susan Duty
Journal:  Br J Pharmacol       Date:  2010-09       Impact factor: 8.739

10.  Discovery of 3-aminopicolinamides as metabotropic glutamate receptor subtype 4 (mGlu4) positive allosteric modulator warheads engendering CNS exposure and in vivo efficacy.

Authors:  Rocco D Gogliotti; Darren W Engers; Pedro M Garcia-Barrantes; Joseph D Panarese; Patrick R Gentry; Anna L Blobaum; Ryan D Morrison; J Scott Daniels; Analisa D Thompson; Carrie K Jones; P Jeffrey Conn; Colleen M Niswender; Craig W Lindsley; Corey R Hopkins
Journal:  Bioorg Med Chem Lett       Date:  2016-04-19       Impact factor: 2.823
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