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  1. Article ; Online: Discovery of a Series of Substituted 1

    Gelin, Christine F / Stenne, Brice / Coate, Heather / Hiscox, Afton / Soyode-Johnson, Akinola / Wall, Jessica L / Lord, Brian / Schoellerman, Jeffrey / Coe, Kevin J / Wang, Kai / Alcázar, Jesus / Chrovian, Christa C / Dvorak, Curt A / Carruthers, Nicholas I / Koudriakova, Tatiana / Balana, Bartosz / Letavic, Michael A

    Journal of medicinal chemistry

    2023  Volume 66, Issue 4, Page(s) 2877–2892

    Abstract: Herein, we describe a series of substituted ... ...

    Abstract Herein, we describe a series of substituted 1
    MeSH term(s) Animals ; Rats ; Brain/metabolism ; Pyrimidines ; Receptors, N-Methyl-D-Aspartate/metabolism ; Structure-Activity Relationship
    Chemical Substances NR2B NMDA receptor ; Pyrimidines ; Receptors, N-Methyl-D-Aspartate
    Language English
    Publishing date 2023-02-09
    Publishing country United States
    Document type Journal Article
    ZDB-ID 218133-2
    ISSN 1520-4804 ; 0022-2623
    ISSN (online) 1520-4804
    ISSN 0022-2623
    DOI 10.1021/acs.jmedchem.2c01916
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  2. Article: 1

    Chrovian, Christa C / Soyode-Johnson, Akinola / Wall, Jessica L / Rech, Jason C / Schoellerman, Jeff / Lord, Brian / Coe, Kevin J / Carruthers, Nicholas I / Nguyen, Leslie / Jiang, Xiaohui / Koudriakova, Tatiana / Balana, Bartosz / Letavic, Michael A

    ACS medicinal chemistry letters

    2019  Volume 10, Issue 3, Page(s) 261–266

    Abstract: Herein, we disclose a series of selective GluN2B negative allosteric modulators containing a ... ...

    Abstract Herein, we disclose a series of selective GluN2B negative allosteric modulators containing a 1
    Language English
    Publishing date 2019-01-10
    Publishing country United States
    Document type Journal Article
    ISSN 1948-5875
    ISSN 1948-5875
    DOI 10.1021/acsmedchemlett.8b00542
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  3. Article ; Online: Design, Synthesis, and Preclinical Evaluation of 3-Methyl-6-(5-thiophenyl)-1,3-dihydro-imidazo[4,5-

    Chrovian, Christa C / Soyode-Johnson, Akinola / Stenne, Brice / Pippel, Daniel J / Schoellerman, Jeffrey / Lord, Brian / Needham, Alexandra S / Xia, Chungfang / Coe, Kevin J / Sepassi, Kia / Schoetens, Freddy / Scott, Brian / Nguyen, Leslie / Jiang, Xiaohui / Koudriakova, Tatiana / Balana, Bartosz / Letavic, Michael A

    Journal of medicinal chemistry

    2020  Volume 63, Issue 17, Page(s) 9181–9196

    Abstract: Selective inhibitors of the GluN2B subunit ... ...

    Abstract Selective inhibitors of the GluN2B subunit of
    MeSH term(s) Allosteric Regulation ; Animals ; Antipsychotic Agents/chemical synthesis ; Antipsychotic Agents/pharmacokinetics ; Antipsychotic Agents/therapeutic use ; Brain/metabolism ; Dogs ; Drug Design ; Drug Evaluation, Preclinical ; Half-Life ; Humans ; Imidazoles/chemistry ; Imidazoles/pharmacokinetics ; Imidazoles/therapeutic use ; Male ; Mood Disorders/drug therapy ; Mood Disorders/pathology ; Nanostructures/chemistry ; Permeability/drug effects ; Pyridines/chemistry ; Pyridines/pharmacokinetics ; Pyridines/therapeutic use ; Rats ; Rats, Sprague-Dawley ; Receptors, N-Methyl-D-Aspartate/antagonists & inhibitors ; Receptors, N-Methyl-D-Aspartate/genetics ; Receptors, N-Methyl-D-Aspartate/metabolism ; Solubility ; Structure-Activity Relationship
    Chemical Substances Antipsychotic Agents ; Imidazoles ; NR2B NMDA receptor ; Pyridines ; Receptors, N-Methyl-D-Aspartate ; imidazo(4,5-b)pyridine
    Language English
    Publishing date 2020-08-28
    Publishing country United States
    Document type Journal Article
    ZDB-ID 218133-2
    ISSN 1520-4804 ; 0022-2623
    ISSN (online) 1520-4804
    ISSN 0022-2623
    DOI 10.1021/acs.jmedchem.9b02113
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  4. Article ; Online: Novel Phenyl-Substituted 5,6-Dihydro-[1,2,4]triazolo[4,3-a]pyrazine P2X7 Antagonists with Robust Target Engagement in Rat Brain.

    Chrovian, Christa C / Soyode-Johnson, Akinola / Ao, Hong / Bacani, Genesis M / Carruthers, Nicholas I / Lord, Brian / Nguyen, Leslie / Rech, Jason C / Wang, Qi / Bhattacharya, Anindya / Letavic, Michael A

    ACS chemical neuroscience

    2016  Volume 7, Issue 4, Page(s) 490–497

    Abstract: Novel 5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazine P2X7 antagonists were optimized to allow for good blood-brain barrier permeability and high P2X7 target engagement in the brain of rats. Compound 25 (huP2X7 IC50 = 9 nM; rat P2X7 IC50 = 42 nM) achieved 80% ...

    Abstract Novel 5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazine P2X7 antagonists were optimized to allow for good blood-brain barrier permeability and high P2X7 target engagement in the brain of rats. Compound 25 (huP2X7 IC50 = 9 nM; rat P2X7 IC50 = 42 nM) achieved 80% receptor occupancy for 6 h when dosed orally at 10 mg/kg in rats as measured by ex vivo radioligand binding autoradiography. Structure-activity relationships within this series are described, as well as in vitro ADME results. In vivo pharmacokinetic data for key compounds is also included.
    MeSH term(s) Animals ; Autoradiography ; Binding, Competitive/drug effects ; Brain/drug effects ; Dose-Response Relationship, Drug ; Humans ; In Vitro Techniques ; Inhibitory Concentration 50 ; Protein Binding/drug effects ; Purinergic P2X Receptor Antagonists/chemistry ; Purinergic P2X Receptor Antagonists/pharmacology ; Pyrazines/chemistry ; Pyrazines/pharmacology ; Rats ; Structure-Activity Relationship
    Chemical Substances Purinergic P2X Receptor Antagonists ; Pyrazines
    Language English
    Publishing date 2016-04-20
    Publishing country United States
    Document type Journal Article
    ISSN 1948-7193
    ISSN (online) 1948-7193
    DOI 10.1021/acschemneuro.5b00303
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  5. Article ; Online: A Dipolar Cycloaddition Reaction To Access 6-Methyl-4,5,6,7-tetrahydro-1H-[1,2,3]triazolo[4,5-c]pyridines Enables the Discovery Synthesis and Preclinical Profiling of a P2X7 Antagonist Clinical Candidate.

    Chrovian, Christa C / Soyode-Johnson, Akinola / Peterson, Alexander A / Gelin, Christine F / Deng, Xiaohu / Dvorak, Curt A / Carruthers, Nicholas I / Lord, Brian / Fraser, Ian / Aluisio, Leah / Coe, Kevin J / Scott, Brian / Koudriakova, Tatiana / Schoetens, Freddy / Sepassi, Kia / Gallacher, David J / Bhattacharya, Anindya / Letavic, Michael A

    Journal of medicinal chemistry

    2017  Volume 61, Issue 1, Page(s) 207–223

    Abstract: A single pot dipolar cycloaddition reaction/Cope elimination sequence was developed to access novel 1,4,6,7-tetrahydro-5H-[1,2,3]triazolo[4,5-c]pyridine P2X7 antagonists that contain a synthetically challenging chiral center. The structure-activity ... ...

    Abstract A single pot dipolar cycloaddition reaction/Cope elimination sequence was developed to access novel 1,4,6,7-tetrahydro-5H-[1,2,3]triazolo[4,5-c]pyridine P2X7 antagonists that contain a synthetically challenging chiral center. The structure-activity relationships of the new compounds are described. Two of these compounds, (S)-(2-fluoro-3-(trifluoromethyl)phenyl)(1-(5-fluoropyrimidin-2-yl)-6-methyl-1,4,6,7-tetrahydro-5H-[1,2,3]triazolo[4,5-c]pyridin-5-yl)methanone (compound 29) and (S)-(3-fluoro-2-(trifluoromethyl)pyridin-4-yl)(1-(5-fluoropyrimidin-2-yl)-6-methyl-1,4,6,7-tetrahydro-5H-[1,2,3]triazolo[4,5-c]pyridin-5-yl)methanone (compound 35), were found to have robust P2X7 receptor occupancy at low doses in rat with ED
    MeSH term(s) Animals ; Cycloaddition Reaction ; Dogs ; Drug Design ; Humans ; Male ; Mice ; Models, Molecular ; Molecular Conformation ; Purinergic P2X Receptor Antagonists/chemical synthesis ; Purinergic P2X Receptor Antagonists/chemistry ; Purinergic P2X Receptor Antagonists/pharmacokinetics ; Purinergic P2X Receptor Antagonists/pharmacology ; Pyridines/chemical synthesis ; Pyridines/chemistry ; Pyridines/pharmacokinetics ; Pyridines/pharmacology ; Rats ; Receptors, Purinergic P2X7/metabolism ; Stereoisomerism ; Tissue Distribution
    Chemical Substances Purinergic P2X Receptor Antagonists ; Pyridines ; Receptors, Purinergic P2X7
    Language English
    Publishing date 2017-12-20
    Publishing country United States
    Document type Journal Article
    ZDB-ID 218133-2
    ISSN 1520-4804 ; 0022-2623
    ISSN (online) 1520-4804
    ISSN 0022-2623
    DOI 10.1021/acs.jmedchem.7b01279
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  6. Article ; Online: Novel substituted pyrrolidines are high affinity histamine H3 receptor antagonists.

    Stocking, Emily M / Aluisio, Leah / Atack, John R / Bonaventure, Pascal / Carruthers, Nicholas I / Dugovic, Christine / Everson, Anita / Fraser, Ian / Jiang, Xiaohui / Leung, Perry / Lord, Brian / Ly, Kiev S / Morton, Kirsten L / Nepomuceno, Diane / Shah, Chandravadan R / Shelton, Jonathan / Soyode-Johnson, Akinola / Letavic, Michael A

    Bioorganic & medicinal chemistry letters

    2010  Volume 20, Issue 9, Page(s) 2755–2760

    Abstract: Pre-clinical characterization of novel substituted pyrrolidines that are high affinity histamine H(3) receptor antagonists is described. These compounds efficiently penetrate the CNS and occupy the histamine H(3) receptor in rat brain following oral ... ...

    Abstract Pre-clinical characterization of novel substituted pyrrolidines that are high affinity histamine H(3) receptor antagonists is described. These compounds efficiently penetrate the CNS and occupy the histamine H(3) receptor in rat brain following oral administration. One compound, (2S,4R)-1-[2-(4-cyclobutyl-[1,4]diazepane-1-carbonyl)-4-(3-fluoro-phenoxy)-pyrrolidin-1-yl]-ethanone, was extensively profiled and shows promise as a potential clinical candidate.
    MeSH term(s) Administration, Oral ; Animals ; Azepines/chemical synthesis ; Azepines/chemistry ; Azepines/pharmacokinetics ; Brain/metabolism ; Dogs ; Drug Evaluation, Preclinical ; Histamine H3 Antagonists/chemical synthesis ; Histamine H3 Antagonists/chemistry ; Histamine H3 Antagonists/pharmacokinetics ; Humans ; Mice ; Pyrrolidines/chemical synthesis ; Pyrrolidines/chemistry ; Pyrrolidines/pharmacokinetics ; Rats ; Receptors, Histamine H3/chemistry ; Receptors, Histamine H3/metabolism ; Structure-Activity Relationship
    Chemical Substances 1-(2-(4-cyclobutyl-(1,4)diazepane-1-carbonyl)-4-(3-fluorophenoxy)pyrrolidin-1-yl)ethanone ; Azepines ; Histamine H3 Antagonists ; Pyrrolidines ; Receptors, Histamine H3
    Language English
    Publishing date 2010-05-01
    Publishing country England
    Document type Journal Article
    ZDB-ID 1063195-1
    ISSN 1464-3405 ; 0960-894X
    ISSN (online) 1464-3405
    ISSN 0960-894X
    DOI 10.1016/j.bmcl.2010.03.071
    Database MEDical Literature Analysis and Retrieval System OnLINE

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