Search Results - "Carcache, David A."

Total Synthesis of (±)-Jiadifenin and Studies Directed to Understanding Its SAR:  Probing Mechanistic and Stereochemical Issues in Palladium-Mediated Allylation of Enolate-Like Structures by Carcache, David A, Cho, Young Shin, Hua, Zihao, Tian, Yuan, Li, Yue-Ming, Danishefsky, Samuel J

“…The total synthesis of jiadifenin has been accomplished. The synthesis allows us to build an SAR profile which suggests that the jiadifenin skeleton may be…”
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Total Synthesis of (±)-Jiadifenin, a Non-peptidyl Neurotrophic Modulator by Cho, Young Shin, Carcache, David A, Tian, Yuan, Li, Yue-Ming, Danishefsky, Samuel J

“…We report the first total synthesis of jiadifenin (1), the establishment of a modality for its biological evaluation, and the discovery of apparently more…”
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Optimizing a Weakly Binding Fragment into a Potent RORγt Inverse Agonist with Efficacy in an in Vivo Inflammation Model by Carcache, David A, Vulpetti, Anna, Kallen, Joerg, Mattes, Henri, Orain, David, Stringer, Rowan, Vangrevelinghe, Eric, Wolf, Romain M, Kaupmann, Klemens, Ottl, Johannes, Dawson, Janet, Cooke, Nigel G, Hoegenauer, Klemens, Billich, Andreas, Wagner, Juergen, Guntermann, Christine, Hintermann, Samuel

“…The transcription factor RORγt is an attractive drug-target due to its role in the differentiation of IL-17 producing Th17 cells that play a critical role in…”
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Synthesis and Biological Evaluation of New Triazolo- and Imidazolopyridine RORγt Inverse Agonists by Hintermann, Samuel, Guntermann, Christine, Mattes, Henri, Carcache, David A., Wagner, Juergen, Vulpetti, Anna, Billich, Andreas, Dawson, Janet, Kaupmann, Klemens, Kallen, Joerg, Stringer, Rowan, Orain, David

“…Retinoic‐acid‐related orphan receptor γt (RORγt) is a key transcription factor implicated in the production of pro‐inflammatory Th17 cytokines, which drive a…”
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Discovery of 1H-pyrrolo[2,3-c]pyridine-7-carboxamides as novel, allosteric mGluR5 antagonists by Koller, Manuel, Carcache, David A., Orain, David, Ertl, Peter, Behnke, Dirk, Desrayaud, Sandrine, Laue, Grit, Vranesic, Ivo

“…1H-pyrrolo[2,3-c]pyridine-7-carboxamides constitute a new series of allosteric mGluR5 antagonists. Variation of the substituents attached to the heterocyclic…”
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Quinazolinedione sulfonamides: A novel class of competitive AMPA receptor antagonists with oral activity by Koller, Manuel, Lingenhoehl, Kurt, Schmutz, Markus, Vranesic, Ivan-Toma, Kallen, Joerg, Auberson, Yves P., Carcache, David A., Mattes, Henri, Ofner, Silvio, Orain, David, Urwyler, Stephan

“…Quinazoline-2,4-diones with a sulfonamide group attached to the N(3) ring atom constitute a novel class of competitive AMPA receptor antagonists. One of the…”
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6-Amino quinazolinedione sulfonamides as orally active competitive AMPA receptor antagonists by Orain, David, Ofner, Silvio, Koller, Manuel, Carcache, David A., Froestl, Wolfgang, Allgeier, Hans, Rasetti, Vittorio, Nozulak, Joachim, Mattes, Henri, Soldermann, Nicolas, Floersheim, Philipp, Desrayaud, Sandrine, Kallen, Joerg, Lingenhoehl, Kurt, Urwyler, Stephan

“…A new set of quinazolinedione sulfonamide derivatives as competitive AMPA receptor antagonist with improved properties compared to 1 is disclosed. By…”
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Development of a New Class of Inhibitors for the Malarial Aspartic Protease Plasmepsin II Based on a Central 7-Azabicyclo[2.2.1]heptane Scaffold by Carcache, David A., Hörtner, Simone R., Seiler, Paul, Diederich, François, Dorn, Arnulf, Märki, Hans Peter, Binkert, Christoph, Bur, Daniel

“…Plasmepsin II (PMII), a malarial aspartic protease involved in the catabolism of hemoglobin in parasites of the genus Plasmodium, and renin, a human aspartic…”
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A New Class of Inhibitors for the Malarial Aspartic Protease Plasmepsin II Based on a Central 11-Azatricyclo[6.2.1.02,7]undeca-2,4,6-triene Scaffold by Carcache, David A., Hörtner, Simone R., Bertogg, Andreas, Diederich, François, Dorn, Arnulf, Märki, Hans Peter, Binkert, Christoph, Bur, Daniel

“…A new class of nonpeptidic inhibitors of the malarial aspartic protease plasmepsin II (PMII) with up to single‐digit micromolar activities (IC50 values) was…”
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The Synthesis and Preliminary Biological Evaluation of a Novel Steroid with Neurotrophic Activity:  NGA0187 by Hua, Zihao, Carcache, David A, Tian, Yuan, Li, Yue-Ming, Danishefsky, Samuel J

“…A full account of the total synthesis of neurotrophic compound NGA0187 is provided. A key feature of the synthesis involved the direct selective oxidation of…”
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De Novo Design, Synthesis, and In Vitro Evaluation of a New Class of Nonpeptidic Inhibitors of the Malarial Enzyme Plasmepsin II by Carcache, David A., Hörtner, Simone R., Bertogg, Andreas, Binkert, Christoph, Bur, Daniel, Märki, Hans Peter, Dorn, Arnulf, Diederich, François

“…Pocket change: A new family of plasmepsin II inhibitors (see scheme) was developed by taking advantage of the putative flexibility of plasmepsin II and…”
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Synthesis and Biological Evaluation of New Triazolo- and Imidazolopyridine ROR[gamma]t Inverse Agonists by Hintermann, Samuel, Guntermann, Christine, Mattes, Henri, Carcache, David A, Wagner, Juergen, Vulpetti, Anna, Billich, Andreas, Dawson, Janet, Kaupmann, Klemens, Kallen, Joerg, Stringer, Rowan, Orain, David

“…Retinoic-acid-related orphan receptor[gamma]t (ROR[gamma]t) is a key transcription factor implicated in the production of pro-inflammatory Th17 cytokines,…”
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Discovery of 1H-pyrrolo[2,3-c]pyridine-7-carboxamides as novel, allosteric mGluRS antagonists by KOLLER, Manuel, CARCACHE, David A, ORAIN, David, ERTL, Peter, BEHNKE, Dirk, DESRAYAUD, Sandrine, LAUE, Grit, VRANESIC, Ivo

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