Literature DB >> 16099654

9H-Xanthene-9-carboxylic acid [1,2,4]oxadiazol-3-yl- and (2H-tetrazol-5-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 based on the lead compound (9H-xanthene-9-carbonyl)-carbamic acid butyl ester derived from random-screening hit diphenylacetyl-carbamic acid ethyl ester were 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 new class of positive allosteric modulators of mGlu1 receptors will be discussed in detail.

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Year:  2005        PMID： 16099654     DOI： 10.1016/j.bmcl.2005.05.135

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


  11 in total

1.  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 2.  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

3.  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

4.  Synthesis of phidianidines A and B.

Authors:  Hong-Yu Lin; Barry B Snider
Journal:  J Org Chem       Date:  2012-05-01       Impact factor: 4.354

5.  Tailored fragments of roseophilin selectively antagonize Mcl-1 in vitro.

Authors:  Jack D Bracken; Andrew D Carlson; James H Frederich; Mai Nguyen; Gordon C Shore; Patrick G Harran
Journal:  Tetrahedron Lett       Date:  2015-06-03       Impact factor: 2.415

6.  Allosteric potentiators of metabotropic glutamate receptor subtype 1a differentially modulate independent signaling pathways in baby hamster kidney cells.

Authors:  Douglas J Sheffler; P Jeffrey Conn
Journal:  Neuropharmacology       Date:  2008-07-02       Impact factor: 5.250

7.  Chemical modulation of mutant mGlu1 receptors derived from deleterious GRM1 mutations found in schizophrenics.

Authors:  Hyekyung P Cho; Pedro M Garcia-Barrantes; John T Brogan; Corey R Hopkins; Colleen M Niswender; Alice L Rodriguez; Daryl F Venable; Ryan D Morrison; Michael Bubser; J Scott Daniels; Carrie K Jones; P Jeffrey Conn; Craig W Lindsley
Journal:  ACS Chem Biol       Date:  2014-08-28       Impact factor: 5.100

Review 8.  Targeting metabotropic glutamate receptors for novel treatments of schizophrenia.

Authors:  James Maksymetz; Sean P Moran; P Jeffrey Conn
Journal:  Mol Brain       Date:  2017-04-26       Impact factor: 4.041

9.  Design, Synthesis, and Functional Evaluation of 1, 5-Disubstituted Tetrazoles as Monoamine Neurotransmitter Reuptake Inhibitors.

Authors:  Suresh Paudel; Shuji Wang; Eunae Kim; Dooti Kundu; Xiao Min; Chan Young Shin; Kyeong-Man Kim
Journal:  Biomol Ther (Seoul)       Date:  2022-03-01       Impact factor: 4.634

10.  Natural phosphate-supported Cu(ii), an efficient and recyclable catalyst for the synthesis of xanthene and 1,4-disubstituted-1,2,3-triazole derivatives.

Authors:  Abbas Amini; Azadeh Fallah; Chun Cheng; Mahmood Tajbakhsh
Journal:  RSC Adv       Date:  2018-12-12       Impact factor: 4.036
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