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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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    In stock of ZB MED Cologne/Königswinter

    Zs.B 151: Show issues Location:
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  2. Article ; Online: Translating New Lung Cancer Screening Guidelines into Practice: The Experience of One Community Hospital.

    Ledford, Christy J W / Gawrys, Breanna L / Wall, Jessica L / Saas, Patrick D / Seehusen, Dean A

    Journal of the American Board of Family Medicine : JABFM

    2016  Volume 29, Issue 1, Page(s) 152–155

    Abstract: Introduction: In December 2013 the US Preventive Services Task Force issued a recommendation for lung cancer screening with annual low-dose computed tomography (LDCT). As screening guidelines emerge and change, this creates an environment for studying ... ...

    Abstract Introduction: In December 2013 the US Preventive Services Task Force issued a recommendation for lung cancer screening with annual low-dose computed tomography (LDCT). As screening guidelines emerge and change, this creates an environment for studying the translation of these guidelines into practice. This study assessed how these guidelines were implemented in a community hospital setting and the resulting radiologic findings.
    Methods: This observational study examined the radiologic outcomes of LDCT lung cancer screening guidelines and the resulting notification.
    Results: During the first year after publication of the guidelines, 94 screening LDCT scans were ordered. Of these, 21 (22.3%) did not meet the criteria outlined by the US Preventive Services Task Force. Among the 72 cases that did met published criteria, 65.3% of scans detected nodules, and among the remaining 35.6%, half had another clinically significant finding.
    Discussion: This study shows that new lung cancer screening guidelines, as implemented at a community hospital, resulted in radiologic findings that required follow-up in more than half of patients. Clinicians must be aware of these potential incidental findings when talking to patients about the decision to order screenings.
    MeSH term(s) Early Detection of Cancer/methods ; Early Detection of Cancer/standards ; Guideline Adherence/statistics & numerical data ; Hospitals, Community/organization & administration ; Humans ; Incidental Findings ; Lung/diagnostic imaging ; Lung Neoplasms/diagnosis ; Lung Neoplasms/diagnostic imaging ; Lung Neoplasms/prevention & control ; Mass Screening/methods ; Mass Screening/organization & administration ; Mass Screening/standards ; Organizational Case Studies ; Practice Guidelines as Topic ; Tomography, X-Ray Computed ; United States
    Language English
    Publishing date 2016-01
    Publishing country United States
    Document type Journal Article ; Observational Study ; Research Support, Non-U.S. Gov't
    ZDB-ID 2239939-2
    ISSN 1558-7118 ; 1557-2625
    ISSN (online) 1558-7118
    ISSN 1557-2625
    DOI 10.3122/jabfm.2016.01.150120
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    Zs.A 2626: Show issues Location:
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  3. 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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  4. Article ; Online: Preclinical characterization of substituted 6,7-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-8(5H)-one P2X7 receptor antagonists.

    Ameriks, Michael K / Ao, Hong / Carruthers, Nicholas I / Lord, Brian / Ravula, Suchitra / Rech, Jason C / Savall, Brad M / Wall, Jessica L / Wang, Qi / Bhattacharya, Anindya / Letavic, Michael A

    Bioorganic & medicinal chemistry letters

    2016  Volume 26, Issue 2, Page(s) 257–261

    Abstract: The synthesis, SAR, and preclinical characterization of a series of substituted 6,7-dihydro[1,2,4]triazolo[4,3]pyrazin-8(5H)-one P2X7 receptor antagonists are described. Optimized leads from this series comprise some of the most potent human P2X7R ... ...

    Abstract The synthesis, SAR, and preclinical characterization of a series of substituted 6,7-dihydro[1,2,4]triazolo[4,3]pyrazin-8(5H)-one P2X7 receptor antagonists are described. Optimized leads from this series comprise some of the most potent human P2X7R antagonists reported to date (IC50s<1nM). They also exhibit sufficient potency and oral bioavailability in rat to enable extensive in vivo profiling. Although many of the disclosed compounds are peripherally restricted, compound 11d is brain penetrant and upon oral administration demonstrated dose-dependent target engagement in rat hippocampus as determined by ex vivo receptor occupancy with radiotracer 5 (ED50=0.8mg/kg).
    MeSH term(s) Animals ; Blood-Brain Barrier/metabolism ; Caco-2 Cells ; Central Nervous System Agents/chemical synthesis ; Central Nervous System Agents/pharmacokinetics ; Central Nervous System Agents/pharmacology ; Hippocampus/metabolism ; Humans ; Microsomes, Liver/metabolism ; Purinergic P2X Receptor Antagonists/chemical synthesis ; Purinergic P2X Receptor Antagonists/pharmacokinetics ; Purinergic P2X Receptor Antagonists/pharmacology ; Pyrazines/chemical synthesis ; Pyrazines/pharmacokinetics ; Pyrazines/pharmacology ; Rats ; Receptors, Purinergic P2X7/metabolism ; Stereoisomerism ; Structure-Activity Relationship ; Triazoles/chemical synthesis ; Triazoles/pharmacokinetics ; Triazoles/pharmacology ; Tritium
    Chemical Substances 7-(2-chloro-3-(trifluoromethyl)benzyl)-6-methyl-3-pyrimidin-2-yl-6,7-dihydro(1,2,4)triazolo(4,3-a)pyrazin-8(5H)-one ; Central Nervous System Agents ; Purinergic P2X Receptor Antagonists ; Pyrazines ; Receptors, Purinergic P2X7 ; Triazoles ; Tritium (10028-17-8)
    Language English
    Publishing date 2016-01-15
    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.2015.12.052
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    Zs.A 3203: Show issues Location:
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  5. Article: A copper(II)-catalyzed, sequential Michael–aldol reaction for the preparation of 1,2-dihydroquinolines

    Wagner, Anna M / Knezevic, Claire E / Wall, Jessica L / Sun, Victoria L / Buss, Joshua A / Allen, LeeAnn T / Wenzel, Anna G

    Tetrahedron letters. 2012 Feb. 15, v. 53, no. 7

    2012  

    Abstract: A copper(II)-catalyzed, sequential Michael addition-aldol condensation reaction of N-carboxybenzyl-protected aminobenzaldehyde with various α,β-unsaturated N-acyl pyrroles is described. Substrate scope was found to include both aryl and aliphatic N-acyl ... ...

    Abstract A copper(II)-catalyzed, sequential Michael addition-aldol condensation reaction of N-carboxybenzyl-protected aminobenzaldehyde with various α,β-unsaturated N-acyl pyrroles is described. Substrate scope was found to include both aryl and aliphatic N-acyl pyrroles as the Michael acceptors, and isolated product yields as high as 93% were observed. The use of acetonitrile as the reaction solvent proved to be crucial for catalysis, both to function as a labile ligand for copper, as well as an agent to minimize hydrolytic catalyst poisoning.
    Keywords acetonitrile ; catalysts ; catalytic activity ; chemical reactions ; chemical structure ; condensation ; copper ; poisoning ; pyrroles ; solvents
    Language English
    Dates of publication 2012-0215
    Size p. 833-836.
    Publishing place Elsevier Ltd
    Document type Article
    ZDB-ID 204287-3
    ISSN 1873-3581 ; 0040-4039
    ISSN (online) 1873-3581
    ISSN 0040-4039
    DOI 10.1016/j.tetlet.2011.12.017
    Database NAL-Catalogue (AGRICOLA)

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    Zs.A 2837: Show issues Location:
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