Structure–activity relationships for the linker in a series of pyridinyl-alkynes that are antagonists of the metabotropic glutamate receptor 5 (mGluR5)

Peter Bach; Karolina Nilsson; Tor Svensson; Udo Bauer; Lance G. Hammerland; Alecia Peterson; Andreas Wållberg; Krister Österlund; David Karis; Maria Boije; David Wensbo

doi:10.1016/j.bmcl.2006.06.078

Structure–activity relationships for the linker in a series of pyridinyl-alkynes that are antagonists of the metabotropic glutamate receptor 5 (mGluR5)

Bioorganic & Medicinal Chemistry Letters ◽

10.1016/j.bmcl.2006.06.078 ◽

2006 ◽

Vol 16 (18) ◽

pp. 4788-4791 ◽

Cited By ~ 16

Author(s):

Peter Bach ◽

Karolina Nilsson ◽

Tor Svensson ◽

Udo Bauer ◽

Lance G. Hammerland ◽

...

Keyword(s):

Glutamate Receptor ◽

Metabotropic Glutamate Receptor ◽

Metabotropic Glutamate Receptor 5 ◽

Structure Activity Relationships ◽

Metabotropic Glutamate ◽

Structure Activity

Download Full-text

Investigating Metabotropic Glutamate Receptor 5 Allosteric Modulator Cooperativity, Affinity, and Agonism: Enriching Structure-Function Studies and Structure-Activity Relationships

Molecular Pharmacology ◽

10.1124/mol.112.080531 ◽

2012 ◽

Vol 82 (5) ◽

pp. 860-875 ◽

Cited By ~ 64

Author(s):

Karen J. Gregory ◽

Meredith J. Noetzel ◽

Jerri M. Rook ◽

Paige N. Vinson ◽

Shaun R. Stauffer ◽

...

Keyword(s):

Structure Function ◽

Glutamate Receptor ◽

Metabotropic Glutamate Receptor ◽

Allosteric Modulator ◽

Metabotropic Glutamate Receptor 5 ◽

Structure Activity Relationships ◽

Metabotropic Glutamate ◽

Structure Activity

Download Full-text

Synthesis, structure–activity relationships and biological evaluation of 4,5,6,7-tetrahydropyrazolopyrazines as metabotropic glutamate receptor 5 negative allosteric modulators

Bioorganic & Medicinal Chemistry Letters ◽

10.1016/j.bmcl.2016.07.019 ◽

2016 ◽

Vol 26 (16) ◽

pp. 3866-3869 ◽

Cited By ~ 3

Author(s):

Wataru Hirose ◽

Yoshihiro Kato ◽

Takayoshi Yamamoto ◽

Momoe Kassai ◽

Makoto Takata ◽

...

Keyword(s):

Glutamate Receptor ◽

Metabotropic Glutamate Receptor ◽

Biological Evaluation ◽

Allosteric Modulators ◽

Metabotropic Glutamate Receptor 5 ◽

Structure Activity Relationships ◽

Metabotropic Glutamate ◽

Structure Activity

Download Full-text

Design, Synthesis, and Structure−Activity Relationships of Novel Bicyclic Azole-amines as Negative Allosteric Modulators of Metabotropic Glutamate Receptor 5

Journal of Medicinal Chemistry ◽

10.1021/jm100736h ◽

2010 ◽

Vol 53 (19) ◽

pp. 7107-7118 ◽

Cited By ~ 19

Author(s):

Douglas F. Burdi ◽

Rachel Hunt ◽

Lei Fan ◽

Tao Hu ◽

Jun Wang ◽

...

Keyword(s):

Glutamate Receptor ◽

Metabotropic Glutamate Receptor ◽

Allosteric Modulators ◽

Design Synthesis ◽

Metabotropic Glutamate Receptor 5 ◽

Structure Activity Relationships ◽

Metabotropic Glutamate ◽

Structure Activity

Download Full-text

Discovery, synthesis, and structure–activity relationships of 2-aminoquinazoline derivatives as a novel class of metabotropic glutamate receptor 5 negative allosteric modulators

Bioorganic & Medicinal Chemistry Letters ◽

10.1016/j.bmcl.2013.06.049 ◽

2013 ◽

Vol 23 (16) ◽

pp. 4493-4500 ◽

Cited By ~ 8

Author(s):

Holger Kubas ◽

Udo Meyer ◽

Bjoern Krueger ◽

Mirko Hechenberger ◽

Maksims Vanejevs ◽

...

Keyword(s):

Glutamate Receptor ◽

Metabotropic Glutamate Receptor ◽

Allosteric Modulators ◽

Metabotropic Glutamate Receptor 5 ◽

Structure Activity Relationships ◽

Metabotropic Glutamate ◽

Structure Activity

Download Full-text

Exploration of Allosteric Agonism Structure–Activity Relationships within an Acetylene Series of Metabotropic Glutamate Receptor 5 (mGlu5) Positive Allosteric Modulators (PAMs): Discovery of 5-((3-Fluorophenyl)ethynyl)-N-(3-methyloxetan-3-yl)picolinamide (ML254)

Journal of Medicinal Chemistry ◽

10.1021/jm401028t ◽

2013 ◽

Vol 56 (20) ◽

pp. 7976-7996 ◽

Cited By ~ 24

Author(s):

Mark Turlington ◽

Meredith J. Noetzel ◽

Aspen Chun ◽

Ya Zhou ◽

Rocco D. Gogliotti ◽

...

Keyword(s):

Glutamate Receptor ◽

Metabotropic Glutamate Receptor ◽

Allosteric Modulators ◽

Metabotropic Glutamate Receptor 5 ◽

Structure Activity Relationships ◽

Metabotropic Glutamate ◽

Acetylene Series ◽

Structure Activity ◽

Positive Allosteric Modulators

Download Full-text

Structure–activity relationships in a novel series of 7-substituted-aryl quinolines and 5-substituted-aryl benzothiazoles at the metabotropic glutamate receptor subtype 5

Bioorganic & Medicinal Chemistry ◽

10.1016/j.bmc.2010.03.053 ◽

2010 ◽

Vol 18 (9) ◽

pp. 3026-3035 ◽

Cited By ~ 14

Author(s):

Peng Zhang ◽

Mu-Fa Zou ◽

Alice L. Rodriguez ◽

P. Jeffrey Conn ◽

Amy Hauck Newman

Keyword(s):

Glutamate Receptor ◽

Metabotropic Glutamate Receptor ◽

Receptor Subtype ◽

Structure Activity Relationships ◽

Metabotropic Glutamate ◽

Structure Activity

Download Full-text

Synthesis and Structure−Activity Relationships of 3-[(2-Methyl-1,3-thiazol-4-yl)ethynyl]pyridine Analogues as Potent, Noncompetitive Metabotropic Glutamate Receptor Subtype 5 Antagonists; Search for Cocaine Medications

Journal of Medicinal Chemistry ◽

10.1021/jm050570f ◽

2006 ◽

Vol 49 (3) ◽

pp. 1080-1100 ◽

Cited By ~ 61

Author(s):

Yasuyoshi Iso ◽

Ewa Grajkowska ◽

Jarda T. Wroblewski ◽

Jared Davis ◽

Nicholas E. Goeders ◽

...

Keyword(s):

Glutamate Receptor ◽

Metabotropic Glutamate Receptor ◽

Receptor Subtype ◽

Structure Activity Relationships ◽

Metabotropic Glutamate ◽

Structure Activity

Download Full-text

Structure-activity relationships of substituted 5H-thiazolo[3,2-a]pyrimidines as group 2 metabotropic glutamate receptor antagonists

Bioorganic & Medicinal Chemistry Letters ◽

10.1016/s0960-894x(99)00227-9 ◽

1999 ◽

Vol 9 (11) ◽

pp. 1573-1576 ◽

Cited By ~ 58

Author(s):

Jürgen Wichmann ◽

Geo Adam ◽

Sabine Kolczewski ◽

Vincent Mutel ◽

Thomas Woltering

Keyword(s):

Glutamate Receptor ◽

Metabotropic Glutamate Receptor ◽

Receptor Antagonists ◽

Structure Activity Relationships ◽

Metabotropic Glutamate ◽

Structure Activity ◽

Glutamate Receptor Antagonists ◽

Group 2

Download Full-text

Synthesis, in Vitro Pharmacology, Structure−Activity Relationships, and Pharmacokinetics of 3-Alkoxy-2-amino-6-fluorobicyclo[3.1.0]hexane-2,6-dicarboxylic Acid Derivatives as Potent and Selective Group II Metabotropic Glutamate Receptor Antagonists

Journal of Medicinal Chemistry ◽

10.1021/jm0400294 ◽

2004 ◽

Vol 47 (18) ◽

pp. 4570-4587 ◽

Cited By ~ 41

Author(s):

Atsuro Nakazato ◽

Kazunari Sakagami ◽

Akito Yasuhara ◽

Hiroshi Ohta ◽

Ryoko Yoshikawa ◽

...

Keyword(s):

Dicarboxylic Acid ◽

Glutamate Receptor ◽

Metabotropic Glutamate Receptor ◽

Receptor Antagonists ◽

Structure Activity Relationships ◽

Metabotropic Glutamate ◽

Structure Activity ◽

Glutamate Receptor Antagonists ◽

In Vitro Pharmacology

Download Full-text

ChemInform Abstract: Structure-Activity Relationships of Substituted 5H-Thiazolo[3,2-a]pyrimidines as Group 2 Metabotropic Glutamate Receptor Antagonists.

ChemInform ◽

10.1002/chin.199936175 ◽

2010 ◽

Vol 30 (36) ◽

pp. no-no

Author(s):

Juergen Wichmann ◽

Geo Adam ◽

Sabine Kolczewski ◽

Vincent Mutel ◽

Thomas Woltering

Keyword(s):

Glutamate Receptor ◽

Metabotropic Glutamate Receptor ◽

Receptor Antagonists ◽

Structure Activity Relationships ◽

Metabotropic Glutamate ◽

Structure Activity ◽

Glutamate Receptor Antagonists ◽

Abstract Structure ◽

Group 2

Download Full-text