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  1. Article ; Online: A knowledge-based, structural-aided discovery of a novel class of 2-phenylimidazo[1,2-a]pyridine-6-carboxamide H-PGDS inhibitors.

    Schulte, Christie A / Deaton, David N / Diaz, Elsie / Do, Young / Gampe, Robert T / Guss, Jeffrey H / Hancock, Ashley P / Hobbs, Heather / Hodgson, Simon T / Holt, Jason / Jeune, Michael R / Kahler, Kirsten M / Kramer, H Fritz / Le, Joelle / Mortenson, Paul N / Musetti, Caterina / Nolte, Robert T / Orband-Miller, Lisa A / Peckham, Gregory E /
    Petrov, Kim G / Pietrak, Beth L / Poole, Chuck / Price, Daniel J / Saxty, Gordon / Shillings, Anthony / Smalley, Terrence L / Somers, Don O / Stewart, Eugene L / Stuart, J Darren / Thomson, Stephen A

    Bioorganic & medicinal chemistry letters

    2021  Volume 47, Page(s) 128113

    Abstract: Through an internal virtual screen at GlaxoSmithKline a distinct class of 2-phenylimidazo[1,2-a]pyridine-6-carboxamide H-PGDS inhibitors were discovered. Careful evaluation of crystal structures and SAR led to a novel, potent, and orally active ... ...

    Abstract Through an internal virtual screen at GlaxoSmithKline a distinct class of 2-phenylimidazo[1,2-a]pyridine-6-carboxamide H-PGDS inhibitors were discovered. Careful evaluation of crystal structures and SAR led to a novel, potent, and orally active imidazopyridine inhibitor of H-PGDS, 20b. Herein, describes the identification of 2 classes of inhibitors, their syntheses, and their challenges.
    MeSH term(s) Dose-Response Relationship, Drug ; Drug Discovery ; Enzyme Inhibitors/chemical synthesis ; Enzyme Inhibitors/chemistry ; Enzyme Inhibitors/pharmacology ; Humans ; Intramolecular Oxidoreductases/antagonists & inhibitors ; Intramolecular Oxidoreductases/metabolism ; Molecular Structure ; Structure-Activity Relationship
    Chemical Substances Enzyme Inhibitors ; Intramolecular Oxidoreductases (EC 5.3.-) ; HPGDS protein, human (EC 5.3.99.2)
    Language English
    Publishing date 2021-05-13
    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.2021.128113
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

    Zs.A 3203: Show issues Location:
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  2. Article: Optimizing Ligand Efficiency of Selective Androgen Receptor Modulators (SARMs).

    Handlon, Anthony L / Schaller, Lee T / Leesnitzer, Lisa M / Merrihew, Raymond V / Poole, Chuck / Ulrich, John C / Wilson, Joseph W / Cadilla, Rodolfo / Turnbull, Philip

    ACS medicinal chemistry letters

    2015  Volume 7, Issue 1, Page(s) 83–88

    Abstract: A series of selective androgen receptor modulators (SARMs) containing the 1-(trifluoromethyl)benzyl alcohol core have been optimized for androgen receptor (AR) potency and drug-like properties. We have taken advantage of the lipophilic ligand efficiency ( ...

    Abstract A series of selective androgen receptor modulators (SARMs) containing the 1-(trifluoromethyl)benzyl alcohol core have been optimized for androgen receptor (AR) potency and drug-like properties. We have taken advantage of the lipophilic ligand efficiency (LLE) parameter as a guide to interpret the effect of structural changes on AR activity. Over the course of optimization efforts the LLE increased over 3 log units leading to a SARM 43 with nanomolar potency, good aqueous kinetic solubility (>700 μM), and high oral bioavailability in rats (83%).
    Language English
    Publishing date 2015-11-19
    Publishing country United States
    Document type Journal Article
    ISSN 1948-5875
    ISSN 1948-5875
    DOI 10.1021/acsmedchemlett.5b00377
    Database MEDical Literature Analysis and Retrieval System OnLINE

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  3. Article ; Online: The exploration of aza-quinolines as hematopoietic prostaglandin D synthase (H-PGDS) inhibitors with low brain exposure.

    Cadilla, Rodolfo / Deaton, David N / Do, Young / Elkins, Patricia A / Ennulat, Daniela / Guss, Jeffrey H / Holt, Jason / Jeune, Michael R / King, Andrew G / Klapwijk, Jan C / Kramer, H Fritz / Kramer, Nicholas J / Laffan, Susan B / Masuria, Paresh I / McDougal, Alan V / Mortenson, Paul N / Musetti, Caterina / Peckham, Gregory E / Pietrak, Beth L /
    Poole, Chuck / Price, Daniel J / Rendina, Alan R / Sati, Girish / Saxty, Gordon / Shearer, Barry G / Shewchuk, Lisa M / Sneddon, Helen F / Stewart, Eugene L / Stuart, J Darren / Thomas, Dean N / Thomson, Stephen A / Ward, Paris / Wilson, Joseph W / Xu, Tiahshun / Youngman, Mark A

    Bioorganic & medicinal chemistry

    2020  Volume 28, Issue 23, Page(s) 115791

    Abstract: GlaxoSmithKline and Astex Pharmaceuticals recently disclosed the discovery of the potent H-PGDS inhibitor GSK2894631A 1a ( ... ...

    Abstract GlaxoSmithKline and Astex Pharmaceuticals recently disclosed the discovery of the potent H-PGDS inhibitor GSK2894631A 1a (IC
    MeSH term(s) Animals ; Aza Compounds/chemistry ; Binding Sites ; Brain/metabolism ; Cell Line, Tumor ; Cell Survival/drug effects ; Crystallography, X-Ray ; Drug Stability ; Enzyme Inhibitors/chemistry ; Enzyme Inhibitors/metabolism ; Enzyme Inhibitors/pharmacology ; Humans ; Intramolecular Oxidoreductases/antagonists & inhibitors ; Intramolecular Oxidoreductases/metabolism ; Kinetics ; Male ; Mice ; Mice, Inbred C57BL ; Molecular Dynamics Simulation ; Muscle, Skeletal/chemistry ; Muscle, Skeletal/metabolism ; Quinolines/chemistry ; Rats ; Structure-Activity Relationship
    Chemical Substances Aza Compounds ; Enzyme Inhibitors ; Quinolines ; Intramolecular Oxidoreductases (EC 5.3.-) ; HPGDS protein, human (EC 5.3.99.2)
    Language English
    Publishing date 2020-10-03
    Publishing country England
    Document type Journal Article
    ZDB-ID 1161284-8
    ISSN 1464-3391 ; 0968-0896
    ISSN (online) 1464-3391
    ISSN 0968-0896
    DOI 10.1016/j.bmc.2020.115791
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

    Zs.A 3815: Show issues Location:
    Je nach Verfügbarkeit (siehe Angabe bei Bestand)
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  4. Article ; Online: Substituted N-{3-[(1,1-dioxido-1,2-benzothiazol-3-yl)(phenyl)amino]propyl}benzamide analogs as potent Kv1.3 ion channel blockers. Part 2.

    Haffner, Curt D / Thomson, Stephen A / Guo, Yu / Petrov, Kimberly / Larkin, Andrew / Banker, Pierette / Schaaf, Gregory / Dickerson, Scott / Gobel, Jeff / Gillie, Dan / Condreay, J Patrick / Poole, Chuck / Carpenter, Tiffany / Ulrich, John

    Bioorganic & medicinal chemistry letters

    2010  Volume 20, Issue 23, Page(s) 6989–6992

    Abstract: We report the synthesis and in vitro activity of a series of novel substituted N-{3-[(1,1-dioxido-1,2-benzothiazol-3-yl)(phenyl)amino]propyl}benzamide analogs. These analogs showed potent inhibitory activity against Kv1.3. Several demonstrated similar ... ...

    Abstract We report the synthesis and in vitro activity of a series of novel substituted N-{3-[(1,1-dioxido-1,2-benzothiazol-3-yl)(phenyl)amino]propyl}benzamide analogs. These analogs showed potent inhibitory activity against Kv1.3. Several demonstrated similar potency to the known Kv1.3 inhibitor PAP-1 when tested under the IonWorks patch clamp assay conditions. Two compounds 13i and 13rr were advanced further as potential tool compounds for in vivo validation studies.
    MeSH term(s) Amides ; Animals ; Benzamides/chemistry ; Benzamides/pharmacology ; Benzothiazoles/chemistry ; Benzothiazoles/pharmacology ; Cell Line ; Humans ; Kv1.3 Potassium Channel/antagonists & inhibitors ; Pancreatitis-Associated Proteins ; Patch-Clamp Techniques ; Rats ; Structure-Activity Relationship
    Chemical Substances Amides ; Benzamides ; Benzothiazoles ; Kv1.3 Potassium Channel ; Pancreatitis-Associated Proteins ; REG3A protein, human
    Language English
    Publishing date 2010-12-01
    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.2010.09.131
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    Zs.A 3203: Show issues Location:
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  5. Article ; Online: The discovery of quinoline-3-carboxamides as hematopoietic prostaglandin D synthase (H-PGDS) inhibitors.

    Deaton, David N / Do, Young / Holt, Jason / Jeune, Michael R / Kramer, H Fritz / Larkin, Andrew L / Orband-Miller, Lisa A / Peckham, Gregory E / Poole, Chuck / Price, Daniel J / Schaller, Lee T / Shen, Ying / Shewchuk, Lisa M / Stewart, Eugene L / Stuart, J Darren / Thomson, Stephen A / Ward, Paris / Wilson, Joseph W / Xu, Tianshun /
    Guss, Jeffrey H / Musetti, Caterina / Rendina, Alan R / Affleck, Karen / Anders, David / Hancock, Ashley P / Hobbs, Heather / Hodgson, Simon T / Hutchinson, Jonathan / Leveridge, Melanie V / Nicholls, Harry / Smith, Ian E D / Somers, Don O / Sneddon, Helen F / Uddin, Sorif / Cleasby, Anne / Mortenson, Paul N / Richardson, Caroline / Saxty, Gordon

    Bioorganic & medicinal chemistry

    2019  Volume 27, Issue 8, Page(s) 1456–1478

    Abstract: With the goal of discovering more selective anti-inflammatory drugs, than COX inhibitors, to attenuate prostaglandin signaling, a fragment-based screen of hematopoietic prostaglandin D synthase was performed. The 76 crystallographic hits were sorted into ...

    Abstract With the goal of discovering more selective anti-inflammatory drugs, than COX inhibitors, to attenuate prostaglandin signaling, a fragment-based screen of hematopoietic prostaglandin D synthase was performed. The 76 crystallographic hits were sorted into similar groups, with the 3-cyano-quinoline 1a (FP IC
    MeSH term(s) Animals ; Drug Discovery ; Enzyme Inhibitors/chemistry ; Enzyme Inhibitors/pharmacokinetics ; Enzyme Inhibitors/pharmacology ; Humans ; Intramolecular Oxidoreductases/antagonists & inhibitors ; Intramolecular Oxidoreductases/chemistry ; Intramolecular Oxidoreductases/metabolism ; Lipocalins/antagonists & inhibitors ; Lipocalins/chemistry ; Lipocalins/metabolism ; Male ; Mice, Inbred C57BL ; Molecular Docking Simulation ; Quinolines/chemistry ; Quinolines/pharmacokinetics ; Quinolines/pharmacology
    Chemical Substances Enzyme Inhibitors ; Lipocalins ; Quinolines ; quinoline-3-carboxamide ; Intramolecular Oxidoreductases (EC 5.3.-) ; prostaglandin R2 D-isomerase (EC 5.3.99.2)
    Language English
    Publishing date 2019-02-11
    Publishing country England
    Document type Journal Article
    ZDB-ID 1161284-8
    ISSN 1464-3391 ; 0968-0896
    ISSN (online) 1464-3391
    ISSN 0968-0896
    DOI 10.1016/j.bmc.2019.02.017
    Database MEDical Literature Analysis and Retrieval System OnLINE

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    In stock of ZB MED Cologne/Königswinter

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