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)
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
Published in Journal of medicinal chemistry (11.10.2012)
Published in Journal of medicinal chemistry (11.10.2012)
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Toward β‑Secretase‑1 Inhibitors with Improved Isoform Selectivity
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
Published in Journal of medicinal chemistry (26.04.2018)
Published in Journal of medicinal chemistry (26.04.2018)
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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
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
Published in Journal of medicinal chemistry (08.11.2012)
Published in Journal of medicinal chemistry (08.11.2012)
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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
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
Published in Nature medicine (07.12.2017)
Published in Nature medicine (07.12.2017)
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Thiophene Bioisosteres of Spirocyclic σ Receptor Ligands. 1. N-Substituted Spiro[piperidine-4,4′-thieno[3,2-c]pyrans]
Oberdorf, Christoph, Schepmann, Dirk, Vela, Jose Miguel, Diaz, Jose Luis, Holenz, Jörg, Wünsch, Bernhard
Published in Journal of medicinal chemistry (23.10.2008)
Published in Journal of medicinal chemistry (23.10.2008)
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Thiophene Bioisosteres of Spirocyclic σ Receptor Ligands: Relationships between Substitution Pattern and σ Receptor Affinity
Oberdorf, Christoph, Schepmann, Dirk, Vela, Jose Miguel, Buschmann, Helmut, Holenz, Jörg, Wünsch, Bernhard
Published in Journal of medicinal chemistry (14.06.2012)
Published in Journal of medicinal chemistry (14.06.2012)
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Biotransformation of two β-secretase inhibitors including ring opening and contraction of a pyrimidine ring
Lindgren, Anders, Eklund, Göran, Turek, Dominika, Malmquist, Jonas, Swahn, Britt-Marie, Holenz, Jörg, von Berg, Stefan, Karlström, Sofia, Bueters, Tjerk
Published in Drug metabolism and disposition (01.05.2013)
Published in Drug metabolism and disposition (01.05.2013)
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Efficacy of selective 5‐HT6 receptor ligands determined by monitoring 5‐HT6 receptor‐mediated cAMP signaling pathways
Romero, Gonzalo, Sánchez, Elisabeth, Pujol, Marta, Pérez, Pilar, Codony, Xavier, Holenz, Jörg, Buschmann, Helmut, Pauwels, Petrus J
Published in British journal of pharmacology (01.08.2006)
Published in British journal of pharmacology (01.08.2006)
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Combination of Two Pharmacophoric Systems: Synthesis and Pharmacological Evaluation of Spirocyclic Pyranopyrazoles with High σ1 Receptor Affinity
Schläger, Torsten, Schepmann, Dirk, Lehmkuhl, Kirstin, Holenz, Jörg, Vela, Jose Miguel, Buschmann, Helmut, Wünsch, Bernhard
Published in Journal of medicinal chemistry (13.10.2011)
Published in Journal of medicinal chemistry (13.10.2011)
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Aminoimidazoles as BACE-1 inhibitors: The challenge to achieve in vivo brain efficacy
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
Published in Bioorganic & medicinal chemistry letters (01.03.2012)
Published in Bioorganic & medicinal chemistry letters (01.03.2012)
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Identification of Novel Indanylsulfonamide Guanylhydrazones as Potent 5-HT6 Serotonin Receptor Antagonists
Mesquida, Neus, López-Pérez, Sara, Dinarès, Immaculada, Frigola, Jordi, Mercè, Ramon, Holenz, Jörg, Pérez, Raquel, Burgueño, Javier, Alcalde, Ermitas
Published in Journal of medicinal chemistry (08.10.2009)
Published in Journal of medicinal chemistry (08.10.2009)
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Synthesis and Biological Evaluation of the 1-Arylpyrazole Class of sigma(1) Receptor Antagonists: Identification of 4-{2-[5-Methyl-1-(naphthalen-2-yl)-1H-pyrazol-3-yloxy]ethyl}morpholine (S1RA, E-52862)
Luis Diaz, Jose, Cuberes, Rosa, Berrocal, Joana, Contijoch, Montserrat, Christmann, Ute, Fernandez, Ariadna, Port, Adriana, Holenz, Jorg, Buschmann, Helmut, Laggner, Christian, Teresa Serafini, Maria, Burgueno, Javier, Zamanillo, Daniel, Merlos, Manuel, Miguel Vela, Jose, Almansa, Carmen
Published in Journal of medicinal chemistry (11.10.2012)
Published in Journal of medicinal chemistry (11.10.2012)
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Journal Article
Epigenetic Drug Discovery
Sippl, Wolfgang, Jung, Manfred, Mannhold, Raimund, Buschmann, Helmut, Holenz, Jörg
Year of Publication 2019
Year of Publication 2019
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Sulfonimidamides as Sulfonamides Bioisosteres: Rational Evaluation through Synthetic, in Vitro, and in Vivo Studies with γ-Secretase Inhibitors
Sehgelmeble, Fernando, Janson, Juliette, Ray, Colin, Rosqvist, Susanne, Gustavsson, Susanne, Nilsson, Linda I., Minidis, Alexander, Holenz, Jörg, Rotticci, Didier, Lundkvist, Johan, Arvidsson, Per I.
Published in ChemMedChem (05.03.2012)
Published in ChemMedChem (05.03.2012)
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First synthesis of the antimalarial naphthylisoquinoline alkaloid dioncophylline C, and its unnatural anti-HIV dimer, jozimine C
Bringmann, Gerhard, Holenz, Jörg, Weirich, Ralf, Rübenacker, Martin, Funke, Christian, Boyd, Michael R., Gulakowski, Robert J., François, Guido
Published in Tetrahedron (01.01.1998)
Published in Tetrahedron (01.01.1998)
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Combination of Two Pharmacophoric Systems: Synthesis and Pharmacological Evaluation of Spirocyclic Pyranopyrazoles with High σ 1 Receptor Affinity
Schläger, Torsten, Schepmann, Dirk, Lehmkuhl, Kirstin, Holenz, Jörg, Vela, Jose Miguel, Buschmann, Helmut, Wünsch, Bernhard
Published in Journal of medicinal chemistry (13.10.2011)
Published in Journal of medicinal chemistry (13.10.2011)
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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
FRANCOIS, G, STEENACKERS, T, AKE ASSI, L, STEGLICH, W, LAMOTTKE, K, HOLENZ, J, BRINGMANN, G
Published in Parasitology research (1987) (01.07.1999)
Published in Parasitology research (1987) (01.07.1999)
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