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Research

Patent Update: Pulmonary-Allergy, Dermatological, Gastrointestinal & Arthritis: The search for inhibitors of the phospholipases A2

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Pages 673-683 | Published online: 29 Feb 2008

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Mark Hess, Alwine Schulze Elfringhoff & Matthias Lehr. (2008) Design and synthesis of 3-pyrrol-3-yl-3H-isobenzofuran-1-ones as inhibitors of human cytosolic phospholipase A2α. Journal of Enzyme Inhibition and Medicinal Chemistry 23:6, pages 946-957.
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Matthias Lehr. (2001) Phospholipase A2 inhibitors in inflammation. Expert Opinion on Therapeutic Patents 11:7, pages 1123-1136.
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Ulrich Tibes. (1997) Phospholipase A2 inhibitors in development. Expert Opinion on Investigational Drugs 6:3, pages 279-298.
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Thomas D Penning, Donald J Fretland & Michael A Stealey. (1995) Patent Update: Pulmonary-Allergy, Dermatological, Gastrointestinal & Arthritis: Anti-inflammatory patent highlights from July 1994 to April 1995. Expert Opinion on Therapeutic Patents 5:7, pages 623-651.
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Articles from other publishers (21)

Xiang-Lin Yang, Yuan Zhou & Xin-Ling Liu. (2013) Hologram quantative structure–activity relationship studies on 1-(5-carboxyindol-1-yl)propan-2-one inhibitors of human cytosolic phospholipase A2α. Medicinal Chemistry Research 23:3, pages 1512-1518.
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MATTHIAS LEHR. 2012. Anti-Inflammatory Drug Discovery. Anti-Inflammatory Drug Discovery 35 57 .
Walburga Hanekamp & Matthias Lehr. (2012) Determination of arachidonic acid by on-line solid-phase extraction HPLC with UV detection for screening of cytosolic phospholipase A2α inhibitors. Journal of Chromatography B 900, pages 79-84.
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Martina Kaptur, Alwine Schulze Elfringhoff & Matthias Lehr. (2011) Structure–activity relationship studies on 1-(5-carboxyindol-1-yl)-propan-2-one inhibitors of human cytosolic phospholipase A2α: Variation of the activated ketone moiety. Bioorganic & Medicinal Chemistry Letters 21:6, pages 1773-1776.
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Hitoshi NakayamaYuka Morita, Hirohiko KimuraKeiichi Ishihara, Satoshi Akiba & Jun'ichi Uenishi. (2011) Synthesis of N-(Trifluoromethyl-2-pyridinyl)arenesulfonamides as an Inhibitor of Secretory Phospholipase A2. Chemical and Pharmaceutical Bulletin 59:6, pages 783-786.
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Stefanie Bovens, Alwine Schulze Elfringhoff, Martina Kaptur, Dirk Reinhardt, Michael Schäfers & Matthias Lehr. (2010) 1-(5-Carboxyindol-1-yl)propan-2-one Inhibitors of Human Cytosolic Phospholipase A 2 α: Effect of Substituents in Position 3 of the Indole Scaffold on Inhibitory Potency, Metabolic Stability, Solubility, and Bioavailability . Journal of Medicinal Chemistry 53:23, pages 8298-8308.
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Andreas Drews, Stefanie Bovens, Kirsten Roebrock, Cord Sunderkötter, Dirk Reinhardt, Michael Schäfers, Andrea van der Velde, Alwine Schulze Elfringhoff, Jörg Fabian & Matthias Lehr. (2010) 1-(5-Carboxyindol-1-yl)propan-2-one Inhibitors of Human Cytosolic Phospholipase A 2 α with Reduced Lipophilicity: Synthesis, Biological Activity, Metabolic Stability, Solubility, Bioavailability, And Topical in Vivo Activity . Journal of Medicinal Chemistry 53:14, pages 5165-5178.
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Stefanie Bovens, Martina Kaptur, Alwine Schulze Elfringhoff & Matthias Lehr. (2009) 1-(5-Carboxyindol-1-yl)propan-2-ones as inhibitors of human cytosolic phospholipase A2α: Synthesis and properties of bioisosteric benzimidazole, benzotriazole and indazole analogues. Bioorganic & Medicinal Chemistry Letters 19:8, pages 2107-2111.
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Cherukupally Praveen, Javvaji Rama Rao, Padi Pratap Reddy, Kaga Mukkanti & Gade Srinivas Reddy. (2009) Facile synthesis of 6‐aryl‐5 H ‐8‐oxa‐4 b , 7‐diaza‐benzo[ a ]azulen‐9‐one derivatives, new tricyclic heterocycles . Journal of Heterocyclic Chemistry 45:4, pages 1083-1087.
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Mark Hess, Alwine Schulze Elfringhoff & Matthias Lehr. (2007) 1-(5-Carboxy- and 5-carbamoylindol-1-yl)propan-2-ones as inhibitors of human cytosolic phospholipase A2α: Bioisosteric replacement of the carboxylic acid and carboxamide moiety. Bioorganic & Medicinal Chemistry 15:8, pages 2883-2891.
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Joachim Ludwig, Stefanie Bovens, Carsten Brauch, Alwine Schulze Elfringhoff & Matthias Lehr. (2006) Design and Synthesis of 1-Indol-1-yl-propan-2-ones as Inhibitors of Human Cytosolic Phospholipase A 2 α . Journal of Medicinal Chemistry 49:8, pages 2611-2620.
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Iain Walters, Colin Bennion, Stephen Connolly, Pamela J Croshaw, Kim Hardy, Paul Hartopp, Clive G Jackson, Sarah J King, Louise Lawrence, Antonio Mete, David Murray, David H Robinson, Linda Stein, Edward Wells & W John Withnall. (2004) Synthesis and evaluation of substrate-mimicking cytosolic phospholipase A 2 inhibitors––reducing the lipophilicity of the arachidonyl chain isostere. Bioorganic & Medicinal Chemistry Letters 14:14, pages 3645-3649.
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Melanie Schmitt & Matthias Lehr. (2004) HPLC assay with UV spectrometric detection for the evaluation of inhibitors of cytosolic phospholipase A2. Journal of Pharmaceutical and Biomedical Analysis 35:1, pages 135-142.
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Melanie Schmitt & Matthias Lehr. (2003) High-performance liquid chromatographic assay with ultraviolet spectrometric detection for the evaluation of inhibitors of secretory phospholipase A2. Journal of Chromatography B 783:2, pages 327-333.
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Klaus Griessbach, Monika Klimt, Alwine Schulze Elfringhoff & Matthias Lehr. (2003) Structure‐Activity Relationship Studies of 1‐Substituted 3‐Dodecanoylindole‐2‐carboxylic Acids as Inhibitors of Cytosolic Phospholipase A 2 ‐Mediated Arachidonic Acid Release in Intact Platelets . Archiv der Pharmazie 335:11-12, pages 547-555.
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Stephen Connolly, Colin Bennion, Sarah Botterell, Pamela J. Croshaw, Catherine Hallam, Kim Hardy, Paul Hartopp, Clive G. Jackson, Sarah J. King, Louise Lawrence, Antonio Mete, David Murray, David H. Robinson, Gillian M. Smith, Linda Stein, Iain Walters, Edward Wells & W. John Withnall. (2002) Design and Synthesis of a Novel and Potent Series of Inhibitors of Cytosolic Phospholipase A 2 Based on a 1,3-Disubstituted Propan-2-one Skeleton . Journal of Medicinal Chemistry 45:6, pages 1348-1362.
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Dietmar Risse, Alwine Schulze Elfringhoff & Matthias Lehr. (2002) Determination of the cell lytic properties of amphiphilic inhibitors of the cytosolic phospholipase A2 against human platelets by measuring the liberation of serotonin with high-performance liquid chromatography and fluorescence detection. Journal of Chromatography B 769:1, pages 185-190.
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Matthias Lehr, Monika Klimt & Alwine Schulze Elfringhoff. (2001) Novel 3-dodecanoylindole-2-carboxylic acid inhibitors of cytosolic phospholipase A2. Bioorganic & Medicinal Chemistry Letters 11:19, pages 2569-2572.
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Matthias Lehr & Alwine Schulze Elfringhoff. (2000) Comparison of the Inhibition of the Cytosolic Phospholipase A2-Mediated Arachidonic Acid Release by Several Indole-2-carboxylic Acids and 3-(Pyrrol-2-yl)propionic Acids in Bovine and in Human Platelets. Archiv der Pharmazie 333:9, pages 312-314.
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Masahiro Fuji, Fumihiko Watanabe,, Yasuhiko Fujii, Hiroshi Hashizume, Takayuki Okuno, Kazuhiro Shirahase, Isao Teshirogi & Mitsuaki Ohtani. (1997) A Stereoselective and Highly Practical Synthesis of Cytosolic Phospholipase A 2 Substrate, 2- S -Arachidonoyl-1- O -hexadecyl- sn -2-thioglycero-3- O -phosphocholine . The Journal of Organic Chemistry 62:20, pages 6804-6809.
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James L. Kerwin, Joanna K. MacKichan, Melinda J. Semon, Alison M. Wiens, Carolyn C. DeRose & Jessica J. Torvik. (1996) Sterol and steryl ester regulation of phospholipase A2 from the mosquito parasiteLagenidium giganteum. Lipids 31:11, pages 1179-1188.
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