Literature DB >> 23142615

Discovery and SAR of a novel series of non-MPEP site mGlu₅ PAMs based on an aryl glycine sulfonamide scaffold.

Alice L Rodriguez1, Ya Zhou, Richard Williams, C David Weaver, Paige N Vinson, Eric S Dawson, Thomas Steckler, Hilde Lavreysen, Claire Mackie, José M Bartolomé, Gregor J Macdonald, J Scott Daniels, Colleen M Niswender, Carrie K Jones, P Jeffrey Conn, Craig W Lindsley, Shaun R Stauffer.   

Abstract

Herein we report the discovery and SAR of a novel series of non-MPEP site metabotropic glutamate receptor 5 (mGlu(5)) positive allosteric modulators (PAMs) based on an aryl glycine sulfonamide scaffold. This series represents a rare non-MPEP site mGlu(5) PAM chemotype.
Copyright © 2012 Elsevier Ltd. All rights reserved.

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Year:  2012        PMID： 23142615      PMCID： PMC3539767          DOI： 10.1016/j.bmcl.2012.10.068

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


  25 in total

1.  Ligand-based structural hypotheses for virtual screening.

Authors:  Ajay N Jain
Journal:  J Med Chem       Date:  2004-02-12       Impact factor: 7.446

Review 2.  Discovery of positive allosteric modulators of metabotropic glutamate receptor subtype 5 (mGluR5).

Authors:  David L Williams; Craig W Lindsley
Journal:  Curr Top Med Chem       Date:  2005       Impact factor: 3.295

3.  Synthesis and SAR of a mGluR5 allosteric partial antagonist lead: unexpected modulation of pharmacology with slight structural modifications to a 5-(phenylethynyl)pyrimidine scaffold.

Authors:  Sameer Sharma; Alice L Rodriguez; P Jeffrey Conn; Craig W Lindsley
Journal:  Bioorg Med Chem Lett       Date:  2008-05-29       Impact factor: 2.823

4.  A novel selective positive allosteric modulator of metabotropic glutamate receptor subtype 5 has in vivo activity and antipsychotic-like effects in rat behavioral models.

Authors:  Gene G Kinney; Julie A O'Brien; Wei Lemaire; Maryann Burno; Denise J Bickel; Michelle K Clements; Tsing-Bau Chen; David D Wisnoski; Craig W Lindsley; Philip R Tiller; Sheri Smith; Marlene A Jacobson; Cyrille Sur; Mark E Duggan; Douglas J Pettibone; P Jeffrey Conn; David L Williams
Journal:  J Pharmacol Exp Ther       Date:  2004-12-17       Impact factor: 4.030

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.  4-aryl piperazine and piperidine amides as novel mGluR5 positive allosteric modulators.

Authors:  Hui Xiong; Todd A Brugel; Michael Balestra; Dean G Brown; Kelly A Brush; Caprice Hightower; Lindsay Hinkley; Valerie Hoesch; James Kang; Gerard M Koether; John P McCauley; Francis M McLaren; Laura M Panko; Thomas R Simpson; Reed W Smith; James M Woods; Becky Brockel; Vijay Chhajlani; Reto A Gadient; Nathan Spear; Linda A Sygowski; Minli Zhang; Jalaj Arora; Nathalie Breysse; Julie M Wilson; Methvin Isaac; Abdelmalik Slassi; Megan M King
Journal:  Bioorg Med Chem Lett       Date:  2010-10-21       Impact factor: 2.823

7.  Discovery of a Novel Chemical Class of mGlu(5) Allosteric Ligands with Distinct Modes of Pharmacology.

Authors:  Alexis S Hammond; Alice L Rodriguez; Steven D Townsend; Colleen M Niswender; Karen J Gregory; Craig W Lindsley; P Jeffrey Conn
Journal:  ACS Chem Neurosci       Date:  2010-08-19       Impact factor: 4.418

8.  Discovery of molecular switches that modulate modes of metabotropic glutamate receptor subtype 5 (mGlu5) pharmacology in vitro and in vivo within a series of functionalized, regioisomeric 2- and 5-(phenylethynyl)pyrimidines.

Authors:  Sameer Sharma; Jeffrey Kedrowski; Jerri M Rook; Randy L Smith; Carrie K Jones; Alice L Rodriguez; P Jeffrey Conn; Craig W Lindsley
Journal:  J Med Chem       Date:  2009-07-23       Impact factor: 7.446

9.  A family of highly selective allosteric modulators of the metabotropic glutamate receptor subtype 5.

Authors:  Julie A O'Brien; Wei Lemaire; Tsing-Bau Chen; Raymond S L Chang; Marlene A Jacobson; Sookhee N Ha; Craig W Lindsley; Hervé J Schaffhauser; Cyrille Sur; Douglas J Pettibone; P Jeffrey Conn; David L Williams
Journal:  Mol Pharmacol       Date:  2003-09       Impact factor: 4.436

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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  8 in total

1.  Identification of Novel Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 5 Acting at Site Distinct from 2-Methyl-6-(phenylethynyl)-pyridine Binding.

Authors:  Mariusz Butkiewicz; Alice L Rodriguez; Shane E Rainey; Joshua Wieting; Vincent B Luscombe; Shaun R Stauffer; Craig W Lindsley; P Jeffrey Conn; Jens Meiler
Journal:  ACS Chem Neurosci       Date:  2019-06-17       Impact factor: 4.418

2.  Molecular Insights into Metabotropic Glutamate Receptor Allosteric Modulation.

Authors:  Karen J Gregory; P Jeffrey Conn
Journal:  Mol Pharmacol       Date:  2015-03-25       Impact factor: 4.436

3.  mGluR5: exploration of orthosteric and allosteric ligand binding pockets and their applications to drug discovery.

Authors:  Christina Mølck; Kasper Harpsøe; David E Gloriam; Jesper M Mathiesen; Søren M Nielsen; Hans Bräuner-Osborne
Journal:  Neurochem Res       Date:  2014-02-04       Impact factor: 3.996

4.  Development of 1H-Pyrazolo[3,4-b]pyridines as Metabotropic Glutamate Receptor 5 Positive Allosteric Modulators.

Authors:  Matthew D Hill; Haiquan Fang; Jeffrey M Brown; Thaddeus Molski; Amy Easton; Xiaojun Han; Regina Miller; Melissa Hill-Drzewi; Lizbeth Gallagher; Michele Matchett; Michael Gulianello; Anand Balakrishnan; Robert L Bertekap; Kenneth S Santone; Valerie J Whiterock; Xiaoliang Zhuo; Joanne J Bronson; John E Macor; Andrew P Degnan
Journal:  ACS Med Chem Lett       Date:  2016-10-03       Impact factor: 4.345

5.  N-aryl piperazine metabotropic glutamate receptor 5 positive allosteric modulators possess efficacy in preclinical models of NMDA hypofunction and cognitive enhancement.

Authors:  K J Gregory; E J Herman; A J Ramsey; A S Hammond; N E Byun; S R Stauffer; J T Manka; S Jadhav; T M Bridges; C D Weaver; C M Niswender; T Steckler; W H Drinkenburg; A Ahnaou; H Lavreysen; G J Macdonald; J M Bartolomé; C Mackie; B J Hrupka; M G Caron; T L Daigle; C W Lindsley; P J Conn; C K Jones
Journal:  J Pharmacol Exp Ther       Date:  2013-08-21       Impact factor: 4.030

Review 6.  Allosteric modulators for the treatment of schizophrenia: targeting glutamatergic networks.

Authors:  Frank S Menniti; Craig W Lindsley; P Jeffrey Conn; Jayvardhan Pandit; Panayiotis Zagouras; Robert A Volkmann
Journal:  Curr Top Med Chem       Date:  2013       Impact factor: 3.295

7.  Tetrahydronaphthyridine and dihydronaphthyridinone ethers as positive allosteric modulators of the metabotropic glutamate receptor 5 (mGlu₅).

Authors:  Mark Turlington; Chrysa Malosh; Jon Jacobs; Jason T Manka; Meredith J Noetzel; Paige N Vinson; Satyawan Jadhav; Elizabeth J Herman; Hilde Lavreysen; Claire Mackie; José M Bartolomé-Nebreda; Susana Conde-Ceide; M Luz Martín-Martín; Han Min Tong; Silvia López; Gregor J MacDonald; Thomas Steckler; J Scott Daniels; C David Weaver; Colleen M Niswender; Carrie K Jones; P Jeffrey Conn; Craig W Lindsley; Shaun R Stauffer
Journal:  J Med Chem       Date:  2014-06-25       Impact factor: 7.446

8.  Rethinking metabotropic glutamate receptor 5 pathological findings in psychiatric disorders: implications for the future of novel therapeutics.

Authors:  Kelly A Newell; Natalie Matosin
Journal:  BMC Psychiatry       Date:  2014-01-28       Impact factor: 3.630
  8 in total

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