Search Results - "Holenz, Jörg"

Synthesis and Biological Evaluation of the 1‑Arylpyrazole Class of σ1 Receptor Antagonists: Identification of 4‑{2-[5-Methyl-1-(naphthalen-2-yl)‑1H‑pyrazol-3-yloxy]ethyl}morpholine (S1RA, E‑52862) by Díaz, José Luis, Cuberes, Rosa, Berrocal, Joana, Contijoch, Montserrat, Christmann, Ute, Fernández, Ariadna, Port, Adriana, Holenz, Jörg, Buschmann, Helmut, Laggner, Christian, Serafini, Maria Teresa, Burgueño, Javier, Zamanillo, Daniel, Merlos, Manuel, Vela, José Miguel, Almansa, Carmen

“…The synthesis and pharmacological activity of a new series of 1-arylpyrazoles as potent σ1 receptor (σ1R) antagonists are reported. The new compounds were…”
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Toward β‑Secretase‑1 Inhibitors with Improved Isoform Selectivity by Johansson, Patrik, Kaspersson, Karin, Gurrell, Ian K, Bäck, Elisabeth, Eketjäll, Susanna, Scott, Clay W, Cebers, Gvido, Thorne, Philip, McKenzie, Michael J, Beaton, Haydn, Davey, Paul, Kolmodin, Karin, Holenz, Jörg, Duggan, Mark E, Budd Haeberlein, Samantha, Bürli, Roland W

“…BACE1 is responsible for the first step in APP proteolysis, leading to toxic Aβ production, and has been indicated to play a key role in the pathogenesis of…”
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Design and Synthesis of β‑Site Amyloid Precursor Protein Cleaving Enzyme (BACE1) Inhibitors with in Vivo Brain Reduction of β‑Amyloid Peptides by Swahn, Britt-Marie, Kolmodin, Karin, Karlström, Sofia, von Berg, Stefan, Söderman, Peter, Holenz, Jörg, Berg, Stefan, Lindström, Johan, Sundström, Marie, Turek, Dominika, Kihlström, Jacob, Slivo, Can, Andersson, Lars, Pyring, David, Rotticci, Didier, Öhberg, Liselotte, Kers, Annika, Bogar, Krisztian, von Kieseritzky, Fredrik, Bergh, Margareta, Olsson, Lise-Lotte, Janson, Juliette, Eketjäll, Susanna, Georgievska, Biljana, Jeppsson, Fredrik, Fälting, Johanna

“…The evaluation of a series of aminoisoindoles as β-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors and the discovery of a clinical…”
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The small molecule CLP257 does not modify activity of the K + -Cl - co-transporter KCC2 but does potentiate GABA A receptor activity by Cardarelli, Ross A, Jones, Karen, Pisella, Lucie I, Wobst, Heike J, McWilliams, Lisa J, Sharpe, Paul M, Burnham, Matthew P, Baker, David J, Chudotvorova, Ilona, Guyot, Justine, Silayeva, Liliya, Morrow, Danielle H, Dekker, Niek, Zicha, Stephen, Davies, Paul A, Holenz, Jörg, Duggan, Mark E, Dunlop, John, Mather, Robert J, Wang, Qi, Medina, Igor, Brandon, Nicholas J, Deeb, Tarek Z, Moss, Stephen J

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Thiophene Bioisosteres of Spirocyclic σ Receptor Ligands. 1. N-Substituted Spiro[piperidine-4,4′-thieno[3,2-c]pyrans] by Oberdorf, Christoph, Schepmann, Dirk, Vela, Jose Miguel, Diaz, Jose Luis, Holenz, Jörg, Wünsch, Bernhard

“…Herein, the synthesis and pharmacological evaluation of thiophene bioisosteres of the highly potent spirocyclic benzopyran 1 are detailed. The synthesis of…”
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Thiophene Bioisosteres of Spirocyclic σ Receptor Ligands: Relationships between Substitution Pattern and σ Receptor Affinity by Oberdorf, Christoph, Schepmann, Dirk, Vela, Jose Miguel, Buschmann, Helmut, Holenz, Jörg, Wünsch, Bernhard

“…On the basis of the 6′,7′-dihydrospiro[piperidine-4,4′-thieno[3,2-c]pyran] framework, a series of more than 30 σ ligands with versatile substituents in 1-,…”
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Biotransformation of two β-secretase inhibitors including ring opening and contraction of a pyrimidine ring by Lindgren, Anders, Eklund, Göran, Turek, Dominika, Malmquist, Jonas, Swahn, Britt-Marie, Holenz, Jörg, von Berg, Stefan, Karlström, Sofia, Bueters, Tjerk

“…Recently, the discovery of the aminoisoindoles as potent and selective inhibitors of β-secretase was reported, including the close structural analogs compound…”
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Efficacy of selective 5‐HT6 receptor ligands determined by monitoring 5‐HT6 receptor‐mediated cAMP signaling pathways by Romero, Gonzalo, Sánchez, Elisabeth, Pujol, Marta, Pérez, Pilar, Codony, Xavier, Holenz, Jörg, Buschmann, Helmut, Pauwels, Petrus J

“…1 Two novel selective 5‐HT6 receptor ligands E‐6801 (6‐chloro‐N‐(3‐(2‐(dimethylamino)ethyl)‐1H‐indol‐5‐yl)imidazo[2,1‐b]thiazole‐5‐sulfonamide) and E‐6837…”
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Combination of Two Pharmacophoric Systems: Synthesis and Pharmacological Evaluation of Spirocyclic Pyranopyrazoles with High σ1 Receptor Affinity by Schläger, Torsten, Schepmann, Dirk, Lehmkuhl, Kirstin, Holenz, Jörg, Vela, Jose Miguel, Buschmann, Helmut, Wünsch, Bernhard

“…The novel class of spirocyclic σ1 ligands 3 (6′,7′-dihydro-1′H-spiro[piperidine-4,4′-pyrano[4,3-c]pyrazoles]) was designed by the combination of the potent σ1…”
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Aminoimidazoles as BACE-1 inhibitors: The challenge to achieve in vivo brain efficacy by Swahn, Britt-Marie, Holenz, Jörg, Kihlström, Jacob, Kolmodin, Karin, Lindström, Johan, Plobeck, Niklas, Rotticci, Didier, Sehgelmeble, Fernando, Sundström, Marie, Berg, Stefan von, Fälting, Johanna, Georgievska, Biljana, Gustavsson, Susanne, Neelissen, Jan, Ek, Margareta, Olsson, Lise-Lotte, Berg, Stefan

“…The evaluation of a series of bicyclic aminoimidazoles as potent BACE-1 inhibitors is described. The crystal structures of compound 14 and compound 23 in…”
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Identification of Novel Indanylsulfonamide Guanylhydrazones as Potent 5-HT6 Serotonin Receptor Antagonists by Mesquida, Neus, López-Pérez, Sara, Dinarès, Immaculada, Frigola, Jordi, Mercè, Ramon, Holenz, Jörg, Pérez, Raquel, Burgueño, Javier, Alcalde, Ermitas

“…Changing the N,N-(dimethylamino)ethyl side chain in the N-[3-(aminoethyl)inden-5-yl]sulfonamide 5-HT6 serotonin receptor agonists 1 by a conformationally rigid…”
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Synthesis and biological evaluation of the 1-arylpyrazole class of σ(1) receptor antagonists: identification of 4-{2-[5-methyl-1-(naphthalen-2-yl)-1H-pyrazol-3-yloxy]ethyl}morpholine (S1RA, E-52862) by Díaz, José Luis, Cuberes, Rosa, Berrocal, Joana, Contijoch, Montserrat, Christmann, Ute, Fernández, Ariadna, Port, Adriana, Holenz, Jörg, Buschmann, Helmut, Laggner, Christian, Serafini, Maria Teresa, Burgueño, Javier, Zamanillo, Daniel, Merlos, Manuel, Vela, José Miguel, Almansa, Carmen

“…The synthesis and pharmacological activity of a new series of 1-arylpyrazoles as potent σ(1) receptor (σ(1)R) antagonists are reported. The new compounds were…”
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Sulfonimidamides as Sulfonamides Bioisosteres: Rational Evaluation through Synthetic, in Vitro, and in Vivo Studies with γ-Secretase Inhibitors by Sehgelmeble, Fernando, Janson, Juliette, Ray, Colin, Rosqvist, Susanne, Gustavsson, Susanne, Nilsson, Linda I., Minidis, Alexander, Holenz, Jörg, Rotticci, Didier, Lundkvist, Johan, Arvidsson, Per I.

“…The proof of the pudding: A proof‐of‐concept study using γ‐secretase inhibitors as a model has shown that sulfonimidamides act as bioisosteres for…”
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First synthesis of the antimalarial naphthylisoquinoline alkaloid dioncophylline C, and its unnatural anti-HIV dimer, jozimine C by Bringmann, Gerhard, Holenz, Jörg, Weirich, Ralf, Rübenacker, Martin, Funke, Christian, Boyd, Michael R., Gulakowski, Robert J., François, Guido

“…The first total synthesis of dioncophylline C, a new antimalarial lead structure, is described. For the directed construction of the stereogenic biaryl axis,…”
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Combination of Two Pharmacophoric Systems: Synthesis and Pharmacological Evaluation of Spirocyclic Pyranopyrazoles with High σ 1 Receptor Affinity by Schläger, Torsten, Schepmann, Dirk, Lehmkuhl, Kirstin, Holenz, Jörg, Vela, Jose Miguel, Buschmann, Helmut, Wünsch, Bernhard

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Vismione H and structurally related anthranoid compounds of natural and synthetic origin as promising drugs against the human malaria parasite Plasmodium falciparum : structure-activity relationships by FRANCOIS, G, STEENACKERS, T, AKE ASSI, L, STEGLICH, W, LAMOTTKE, K, HOLENZ, J, BRINGMANN, G

“…Natural and synthetic anthranoid compounds were subjected to an evaluation against asexual erythrocytic stages of the human malaria parasite Plasmodium…”
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Medicinal chemistry strategies to 5-HT6 receptor ligands as potential cognitive enhancers and antiobesity agents by HOLENZ, Jörg, PAUWELS, Petrus J, DIAZ, José Luis, MERCE, Ramon, CODONY, Xavier, BUSCHMANN, Helmut

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The small molecule CLP257 does not modify activity of the K+–Cl− co-transporter KCC2 but does potentiate GABAA receptor activity by Cardarelli, Ross A, Jones, Karen, Pisella, Lucie I, Wobst, Heike J, McWilliams, Lisa J, Sharpe, Paul M, Burnham, Matthew P, Baker, David J, Chudotvorova, Ilona, Guyot, Justine, Silayeva, Liliya, Morrow, Danielle H, Dekker, Niek, Zicha, Stephen, Davies, Paul A, Holenz, Jörg, Duggan, Mark E, Dunlop, John, Mather, Robert J, Wang, Qi, Medina, Igor, Brandon, Nicholas J, Deeb, Tarek Z, Moss, Stephen J

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Chronic 5‐HT6 receptor modulation by E‐6837 induces hypophagia and sustained weight loss in diet‐induced obese rats by Fisas, Angels, Codony, Xavier, Romero, Gonzalo, Dordal, Alberto, Giraldo, Jesus, Mercé, Ramon, Holenz, Jörg, Heal, David, Buschmann, Helmut, Pauwels, Petrus Johan

“…1 E‐6837 is a novel, selective and high‐affinity 5‐HT6 receptor ligand (pKi: 9.13) which in vitro demonstrates partial agonism at a presumably silent rat 5‐HT6…”
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Microwave assisted synthesis of spirocyclic pyrrolidines –σ1 receptor ligands with modified benzene-N-distance by Jasper, Annemarie, Schepmann, Dirk, Lehmkuhl, Kirstin, Vela, Jose Miguel, Buschmann, Helmut, Holenz, Jörg, Wünsch, Bernhard

“…Two series of σ1 ligands with a spiro[[2]benzopyran-1,3′-pyrrolidine] (3) and a spiro[[2]benzofuran-1,3′-pyrrolidine] (4) framework were synthesized and…”
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