Literature DB >> 19233648

Fluorinated 9H-xanthene-9-carboxylic acid oxazol-2-yl-amides as potent, orally available mGlu1 receptor enhancers.

Eric Vieira1, Jörg Huwyler, Synèse Jolidon, Frédéric Knoflach, Vincent Mutel, Jürgen Wichmann.   

Abstract

Small molecule mGluR1 enhancers, which are 9H-xanthene-9-carboxylic acid [1,2,4]oxadiazol-3-yl- and (2H-tetrazol-5-yl)-amides, have been previously reported. Fluorinated 9H-xanthene-9-carboxylic acid oxazol-2-yl-amides with improved pharmacokinetic properties have been designed and synthesized as useful pharmacological tools for the study of the physiological roles mediated by mGlu1 receptors. The synthesis and the structure-activity relationship of this class of positive allosteric modulators of mGlu1 receptors will be discussed in detail.

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Year:  2009        PMID： 19233648     DOI： 10.1016/j.bmcl.2009.01.108

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


  18 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.  Development of Novel, CNS Penetrant Positive Allosteric Modulators for the Metabotropic Glutamate Receptor Subtype 1 (mGlu1), Based on an N-(3-Chloro-4-(1,3-dioxoisoindolin-2-yl)phenyl)-3-methylfuran-2-carboxamide Scaffold, That Potentiate Wild Type and Mutant mGlu1 Receptors Found in Schizophrenics.

Authors:  Pedro M Garcia-Barrantes; Hyekyung P Cho; Colleen M Niswender; Frank W Byers; Charles W Locuson; Anna L Blobaum; Zixiu Xiang; Jerri M Rook; P Jeffrey Conn; Craig W Lindsley
Journal:  J Med Chem       Date:  2015-10-08       Impact factor: 7.446

Review 3.  Practical Strategies and Concepts in GPCR Allosteric Modulator Discovery: Recent Advances with Metabotropic Glutamate Receptors.

Authors:  Craig W Lindsley; Kyle A Emmitte; Corey R Hopkins; Thomas M Bridges; Karen J Gregory; Colleen M Niswender; P Jeffrey Conn
Journal:  Chem Rev       Date:  2016-02-16       Impact factor: 60.622

4.  Head-to head comparison of mGlu1 and mGlu5 receptor activation in chronic treatment of absence epilepsy in WAG/Rij rats.

Authors:  V D'Amore; I Santolini; R Celli; L Lionetto; A De Fusco; M Simmaco; C M van Rijn; E Vieira; S R Stauffer; P J Conn; P Bosco; F Nicoletti; G van Luijtelaar; R T Ngomba
Journal:  Neuropharmacology       Date:  2014-05-20       Impact factor: 5.250

5.  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

6.  Lead optimization of the VU0486321 series of mGlu1 PAMs. Part 1: SAR of modifications to the central aryl core.

Authors:  Pedro M Garcia-Barrantes; Hyekyung P Cho; Anna L Blobaum; Colleen M Niswender; P Jeffrey Conn; Craig W Lindsley
Journal:  Bioorg Med Chem Lett       Date:  2015-10-09       Impact factor: 2.823

Review 7.  Progress toward advanced understanding of metabotropic glutamate receptors: structure, signaling and therapeutic indications.

Authors:  Shen Yin; Colleen M Niswender
Journal:  Cell Signal       Date:  2014-05-02       Impact factor: 4.315

Review 8.  mGlu1 receptor as a drug target for treatment of substance use disorders: time to gather stones together?

Authors:  Olga A Dravolina; Edwin Zvartau; Wojciech Danysz; Anton Y Bespalov
Journal:  Psychopharmacology (Berl)       Date:  2017-03-11       Impact factor: 4.530

9.  Re-exploration of the mGlu₁ PAM Ro 07-11401 scaffold: Discovery of analogs with improved CNS penetration despite steep SAR.

Authors:  Pedro M Garcia-Barrantes; Hyekyung P Cho; Tahj M Starr; Anna L Blobaum; Colleen M Niswender; P Jeffrey Conn; Craig W Lindsley
Journal:  Bioorg Med Chem Lett       Date:  2016-03-14       Impact factor: 2.823

10.  Lead optimization of the VU0486321 series of mGlu(1) PAMs. Part 2: SAR of alternative 3-methyl heterocycles and progress towards an in vivo tool.

Authors:  Pedro M Garcia-Barrantes; Hyekyung P Cho; Adam M Metts; Anna L Blobaum; Colleen M Niswender; P Jeffrey Conn; Craig W Lindsley
Journal:  Bioorg Med Chem Lett       Date:  2016-01-02       Impact factor: 2.823
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