Brömmel K, Maskri S, Maisuls I, Konken CP, Rieke M, Petho Z, Strassert CA, Koch O, Schwab A, Wunsch B. Synthesis of Small-Molecule Fluorescent Probes for the In Vitro Imaging of Calcium-Activated Potassium Channel KCa 31. Angew Chem Int Ed Engl 2020;59: 8277-8284. Abstract
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Schepmann D, Neue C, Westphalinger S, Muller C, Bracher F, Lange C, Bednarski P, Almansa C, Friedland K, Rabiger V, Dufer M, Wunsch B. Pharmacological characterization of high-affinity sigma1 receptor ligands with spirocyclic thienopyran and thienofuran scaffold. J Pharm Pharmacol 2020;72: 236-248. Abstract
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Tangherlini G, Borgel F, Schepmann D, Slocum S, Che T, Wagner S, Schwegmann K, Hermann S, Mykicki N, Loser K, Wunsch B. Synthesis and Pharmacological Evaluation of Fluorinated Quinoxaline-Based kappa-Opioid Receptor (KOR) Agonists Designed for PET Studies. Chemmedchem 2020;15: 1834-1853. Abstract
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Baumeister S, Schepmann D, Wunsch B. Synthesis and receptor binding of thiophene bioisosteres of potent GluN2B ligands with a benzo[7]annulene-scaffold. MedChemComm. 2019;10: 315-325. Abstract
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Bergkemper M, Kronenberg E, Schepmann D, Ludwig F-A, Brust P, Wunsch B. Structure-Affinity Relationships of Fluorinated Spirocyclic sigma2 Receptor Ligands with an Exocyclic Benzylamino Moiety. ChemMedChem 2019;14: 1392-1402. Abstract
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Borgel F, Galla F, Lehmkuhl K, Schepmann D, Ametamey SM, Wunsch B. Pharmacokinetic properties of enantiomerically pure GluN2B selective NMDA receptor antagonists with 3-benzazepine scaffold. J Pharm Biomed Anal 2019;172: 214-222. Abstract
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Bunse P, Schlepphorst C, Glorius F, Kitamura M, Wunsch B. Short and Atom-Economic Enantioselective Synthesis of the sigma1-Receptor Ligands (S)- and (R)-Fluspidine-Important Tools for Positron Emission Tomography Studies. J Org Chem 2019;84: 13744-13754. Abstract
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Kronenberg E, Weber F, Brune S, Schepmann D, Almansa C, Friedland K, Laurini E, Pricl S, Wunsch B. Synthesis and Structure-Affinity Relationships of Spirocyclic Benzopyrans with Exocyclic Amino Moiety. J Med Chem 2019;62: 4204-4217. Abstract
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Tangherlini G, Kalinin DV, Schepmann D, Che T, Mykicki N, Stander S, Loser K, Wunsch B. Development of Novel Quinoxaline-Based kappa-Opioid Receptor Agonists for the Treatment of Neuroinflammation. J Med Chem 2019;62: 893-907. Abstract
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Temme L, Borgel F, Schepmann D, Robaa D, Sippl W, Daniliuc C, Wunsch B. Impact of hydroxy moieties at the benzo[7]annulene ring system of GluN2B ligands: Design, synthesis and biological evaluation. Bioorg Med Chem 2019;27: 115146. Abstract
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Thum S, Schepmann D, Ayet E, Pujol M, Nieto FR, Ametamey SM, Wunsch B. Tetrahydro-3-benzazepines with fluorinated side chains as NMDA and sigma1 receptor antagonists: Synthesis, receptor affinity, selectivity and antiallodynic activity. Eur J Med Chem 2019;177: 47-62. Abstract
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Thum S, Schepmann D, Reinoso RF, Alvarez I, Ametamey SM, Wunsch B. Synthesis and pharmacological evaluation of fluorinated benzo[7]annulen-7-amines as GluN2B-selective NMDA receptor antagonists. J Labelled Comp Radiopharm 2019;62: 354-379. Abstract
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Wagner M, Schepmann D, Ametamey SM, Wunsch B. Modification of the 4-phenylbutyl side chain of potent 3-benzazepine-based GluN2B receptor antagonists. Bioorg Med Chem 2019;27: 3559-3567. Abstract
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Bergkemper M, Kronenberg E, Thum S, Borgel F, Daniliuc C, Schepmann D, Nieto FR, Brust P, Reinoso RF, Alvarez I, Wunsch B. Synthesis, Receptor Affinity, and Antiallodynic Activity of Spirocyclic sigma Receptor Ligands with Exocyclic Amino Moiety. J Med Chem 2018;61: 9666-9690. Abstract
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Borgel F, Szermerski M, Schreiber JA, Temme L, Strutz-Seebohm N, Lehmkuhl K, Schepmann D, Ametamey SM, Seebohm G, Schmidt TJ, Wunsch B. Synthesis and Pharmacological Evaluation of Enantiomerically Pure GluN2B Selective NMDA Receptor Antagonists. ChemMedChem 2018;13: 1580-1587. Abstract
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Bunse P, Würthwein E-U, Wünsch B. Synthesis of Substituted 1-Alkylidenephthalanes via Lithium-Promoted 5-exo-dig Cyclization. Eur. J. Org. Chem. 2018: 1806-1812. Abstract
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Butsch V, Borgel F, Galla F, Schwegmann K, Hermann S, Schafers M, Riemann B, Wunsch B, Wagner S. Design, (Radio)Synthesis, and in Vitro and in Vivo Evaluation of Highly Selective and Potent Matrix Metalloproteinase 12 (MMP-12) Inhibitors as Radiotracers for Positron Emission Tomography. J Med Chem 2018;61: 4115-4134. Abstract
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Dey S, Schepmann D, Wunsch B. 2-Methyltetrahydro-3-benzazepin-1-ols - The missing link in SAR of GluN2B selective NMDA receptor antagonists. Bioorg Med Chem 2018;26: 501-508. Abstract
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Fanter L, Schepmann D, Wunsch B. Solid-phase organic synthesis of chiral, non-racemic 1,2,4-trisubstituted 1,4-diazepanes with high sigma1 receptor affinity. Arch Pharm (Weinheim) 2018;351: e1700334. Abstract
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Heimann D, Borgel F, de Vries H, Bachmann K, Rose VE, Frehland B, Schepmann D, Heitman LH, Wunsch B. Optimization of pharmacokinetic properties by modification of a carbazole-based cannabinoid receptor subtype 2 (CB2) ligand. Eur J Med Chem 2018;143: 1436-1447. Abstract
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Heimann D, Borgel F, de Vries H, Patberg M, Jan-Smith E, Frehland B, Schepmann D, Heitman LH, Wunsch B. Optimization of the metabolic stability of a fluorinated cannabinoid receptor subtype 2 (CB2) ligand designed for PET studies. Eur J Med Chem 2018;146: 409-422. Abstract
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Schreiber JA, Müller SL, Westphälinger SE, Schepmann D, Strutz-Seebohm N, Seebohm G, Wünsch B. Systematic variation of the benzoylhydrazine moiety of the GluN2A selective NMDA receptor antagonist TCN-201. Eur J Med Chem 2018;158: 259-269. Abstract
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Szermerski M, Borgel F, Schepmann D, Haider A, Betzel T, Ametamey SM, Wunsch B. Fluorinated GluN2B Receptor Antagonists with a 3-Benzazepine Scaffold Designed for PET Studies. ChemMedChem 2018;13: 1058-1068. Abstract
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Temme L, Frehland B, Schepmann D, Robaa D, Sippl W, Wunsch B. Hydroxymethyl bioisosteres of phenolic GluN2B-selective NMDA receptor antagonists: Design, synthesis and pharmacological evaluation. Eur J Med Chem 2018;144: 672-681. Abstract
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Temme L, Schepmann D, Schreiber JA, Frehland B, Wunsch B. Comparative Pharmacological Study of Common NMDA Receptor Open Channel Blockers Regarding Their Affinity and Functional Activity toward GluN2A and GluN2B NMDA Receptors. ChemMedChem 2018;13: 446-452. Abstract
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Thum S, Schepmann D, Kalinin DV, Ametamey SM, Wunsch B. Replacement of the Benzylpiperidine Moiety with Fluorinated Phenylalkyl Side Chains for the Development of GluN2B Receptor Ligands. ChemMedChem 2018;13: 2522-2529. Abstract
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Torres-Gomez H, Daniliuc C, Schepmann D, Wunsch B. Synthesis of 3-aza[443]propellanes with high sigma1 receptor affinity. Bioorg Med Chem 2018;26: 1705-1712. Abstract
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Zscherp R, Baumeister S, Schepmann D, Wunsch B. Pyridine bioisosteres of potent GluN2B subunit containing NMDA receptor antagonists with benzo[7]annulene scaffold. Eur J Med Chem 2018;157: 397-404. Abstract
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Asare-Nkansah S, Schepmann D, Wunsch B. Synthesis of conformationally restricted 1,3-dioxanes to analyze the bioactive conformation of 1,3-dioxane-based sigma1 and PCP receptor antagonists. Bioorg Med Chem 2017;25: 2472-2481. Abstract
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Dey S, Temme L, Schreiber JA, Schepmann D, Frehland B, Lehmkuhl K, Strutz-Seebohm N, Seebohm G, Wunsch B. Deconstruction - reconstruction approach to analyze the essential structural elements of tetrahydro-3-benzazepine-based antagonists of GluN2B subunit containing NMDA receptors. Eur J Med Chem 2017;138: 552-564. Abstract
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Fanter L, Muller C, Schepmann D, Bracher F, Wunsch B. Chiral-pool synthesis of 1,2,4-trisubstituted 1,4-diazepanes as novel sigma1 receptor ligands. Bioorg Med Chem 2017;25: 4778-4799. Abstract
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Gawaskar S, Temme L, Schreiber JA, Schepmann D, Bonifazi A, Robaa D, Sippl W, Strutz-Seebohm N, Seebohm G, Wunsch B. Design, Synthesis, Pharmacological Evaluation and Docking Studies of GluN2B-Selective NMDA Receptor Antagonists with a Benzo[7]annulen-7-amine Scaffold. ChemMedChem 2017;12: 1212-1222. Abstract
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Heimann D, Lueg C, de Vries H, Frehland B, Schepmann D, Heitman LH, Wunsch B. Bioisosteric replacement of central 1,2,4-oxadiazole ring of high affinity CB2 ligands by regioisomeric 1,3,4-oxadiazole ring. MedChemComm. 2017;8: 1697-1705. Abstract
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Knappmann I, Lehmkuhl K, Kohler J, Schepmann D, Giera M, Bracher F, Wunsch B. Lipase-catalyzed kinetic resolution as key step in the synthesis of enantiomerically pure sigma ligands with 2-benzopyran structure. Bioorg Med Chem 2017;25: 3384-3395. Abstract
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Kokornaczyk AK, Schepmann D, Yamaguchi J, Itami K, Laurini E, Fermeglia M, Pricl S, Wunsch B. Thiazole-Based sigma1 Receptor Ligands: Diversity by Late-Stage C-H Arylation of Thiazoles, Structure-Affinity and Selectivity Relationships, and Molecular Interactions. ChemMedChem 2017;12: 1070-1080. Abstract
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Kokornaczyk AK, Thum S, Daniliuc CG, Junker A, Wünsch B. Molecular structure of a brominated 2-benzazepinone – a crucial intermediate in the synthesis of novel chemokine CCR2 receptor antagonists. Z. Naturforsch. B 2017;72: 421-424. Abstract
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Muller SL, Schreiber JA, Schepmann D, Strutz-Seebohm N, Seebohm G, Wunsch B. Systematic variation of the benzenesulfonamide part of the GluN2A selective NMDA receptor antagonist TCN-201. Eur J Med Chem 2017;129: 124-134. Abstract
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Ortmeyer CP, Haufe G, Schwegmann K, Hermann S, Schafers M, Borgel F, Wunsch B, Wagner S, Hugenberg V. Synthesis and evaluation of a [18F]BODIPY-labeled caspase-inhibitor. Bioorg Med Chem 2017;25: 2167-2176. Abstract
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Rath S, Schepmann D, Wunsch B. Replacement of benzylic hydroxy group by vinyl or hydroxymethyl moiety at the 3-benzazepine scaffold retaining GluN2B affinity. Bioorg Med Chem 2017;25: 5365-5372. Abstract
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Shuto Y, Thum S, Temme L, Schepmann D, Kitamura M, Wunsch B. Do GluN2B subunit containing NMDA receptors tolerate a fluorine atom in the phenylalkyl side chain?. Medchemcomm 2017;8: 975-981. Abstract
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Soeberdt M, Molenveld P, Storcken RPM, Bouzanne des Mazery R, Sterk GJ, Autar R, Bolster MG, Wagner C, Aerts SNH, van Holst FR, Wegert A, Tangherlini G, Frehland B, Schepmann D, Metze D, Lotts T, Knie U, Lin K-Y, Huang T-Y, Lai C-C, Stander S, Wunsch B, Abels C. Design and Synthesis of Enantiomerically Pure Decahydroquinoxalines as Potent and Selective kappa-Opioid Receptor Agonists with Anti-Inflammatory Activity in Vivo. J Med Chem 2017;60: 2526-2551. Abstract
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Thum S, Kokornaczyk AK, Seki T, De Maria M, Ortiz Zacarias NV, de Vries H, Weiss C, Koch M, Schepmann D, Kitamura M, Tschammer N, Heitman LH, Junker A, Wunsch B. Synthesis and biological evaluation of chemokine receptor ligands with 2-benzazepine scaffold. Eur J Med Chem 2017;135: 401-413. Abstract
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Weber F, Brust P, Laurini E, Pricl S, Wunsch B. Fluorinated PET Tracers for Molecular Imaging of sigma1 Receptors in the Central Nervous System. Adv Exp Med Biol 2017;964: 31-48. Abstract
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Wittig C, Schepmann D, Soeberdt M, Daniliuc CG, Wunsch B. Stereoselective synthesis of conformationally restricted KOR agonists based on the 2,5-diazabicyclo[222]octane scaffold. Org Biomol Chem 2017;15: 6520-6540. Abstract
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Hugenberg V, Hermann S, Galla F, Schafers M, Wunsch B, Kolb HC, Szardenings K, Lebedev A, Walsh JC, Mocharla VP, Gangadharmath UB, Kopka K, Wagner S. Radiolabeled hydroxamate-based matrix metalloproteinase inhibitors: How chemical modifications affect pharmacokinetics and metabolic stability. Nucl Med Biol 2016;43: 424-437. Abstract
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Stucke-Ring J, Ronnacker J, Brand C, Holtke C, Schliemann C, Kessler T, Schmidt LH, Harrach S, Mantke V, Hintelmann H, Hartmann W, Wardelmann E, Lenz G, Wunsch B, Muller-Tidow C, Mesters RM, Schwoppe C, Berdel WE. Combinatorial effects of doxorubicin and retargeted tissue factor by intratumoral entrapment of doxorubicin and proapoptotic increase of tumor vascular infarction. Oncotarget 2016;7: 82458-82472. Abstract
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Weber F, Brune S, Borgel F, Lange C, Korpis K, Bednarski PJ, Laurini E, Fermeglia M, Pricl S, Schepmann D, Wunsch B. Rigidity versus Flexibility: Is This an Issue in sigma1 Receptor Ligand Affinity and Activity?. J Med Chem 2016;59: 5505-5519. Abstract
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Wiese C, Grosse Maestrup E, Galla F, Schepmann D, Hiller A, Fischer S, Ludwig F-A, Deuther-Conrad W, Donat CK, Brust P, Buter L, Karst U, Wunsch B. Comparison of in Silico, Electrochemical, in Vitro and in Vivo Metabolism of a Homologous Series of (Radio)fluorinated σ1 Receptor Ligands Designed for Positron Emission Tomography. ChemMedChem 2016;11: 2445–2458. Abstract
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Junker A, Kokornaczyk AK, Zweemer AJM, Frehland B, Schepmann D, Yamaguchi J, Itami K, Faust A, Hermann S, Wagner S, Schafers M, Koch M, Weiss C, Heitman LH, Kopka K, Wunsch B. Synthesis, binding affinity and structure-activity relationships of novel, selective and dual targeting CCR2 and CCR5 receptor antagonists. Org Biomol Chem 2015;13: 2407-2422. Abstract
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Quick MP, Frohlich R, Schepmann D, Wunsch B. Asymmetric synthesis of 3-substituted tetrahydro-2-benzazepines. Org Biomol Chem 2015;13: 7265-7281. Abstract
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Strunz AK, Zweemer AJM, Weiss C, Schepmann D, Junker A, Heitman LH, Koch M, Wunsch B. Synthesis and biological evaluation of spirocyclic antagonists of CCR2 (chemokine CC receptor subtype 2). Bioorg Med Chem 2015;23: 4034-4049. Abstract
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Bourgeois C, Werfel E, Galla F, Lehmkuhl K, Torres-Gomez H, Schepmann D, Kogel B, Christoph T, Strassburger W, Englberger W, Soeberdt M, Huwel S, Galla H-J, Wunsch B. Synthesis and pharmacological evaluation of 5-pyrrolidinylquinoxalines as a novel class of peripherally restricted kappa-opioid receptor agonists. J Med Chem 2014;57: 6845-6860. Abstract
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Brust P, Deuther-Conrad W, Lehmkuhl K, Jia H, Wunsch B. Molecular imaging of sigma1 receptors in vivo: current status and perspectives. Curr Med Chem 2014;21: 35-69. Abstract
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Gawaskar S, Schepmann D, Bonifazi A, Wunsch B. Synthesis, GluN2B affinity and selectivity of benzo[7]annulen-7-amines. Bioorg Med Chem 2014;22: 6638-6646. Abstract
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Hasebein P, Frehland B, Lehmkuhl K, Frohlich R, Schepmann D, Wunsch B. Synthesis and pharmacological evaluation of like- and unlike-configured tetrahydro-2-benzazepines with the alpha-substituted benzyl moiety in the 5-position. Org Biomol Chem 2014;12: 5407-5426. Abstract
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Hasebein P, Frehland B, Schepmann D, Wunsch B. Synthesis, sigma receptor affinity, and pharmacological evaluation of 5-phenylsulfanyl- and 5-benzyl-substituted tetrahydro-2-benzazepines. ChemMedChem 2014;9: 1697-1703. Abstract
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Holl K, Schepmann D, Fischer S, Ludwig F-A, Hiller A, Donat CK, Deuther-Conrad W, Brust P, Wunsch B. Asymmetric Synthesis of Spirocyclic 2-Benzopyrans for Positron Emission Tomography of sigma1 Receptors in the Brain. Pharmaceuticals (Basel) 2014;7: 78-112. Abstract
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Holla K, Schepmann D, Daniliuc CG, Wünsch B. Sharpless asymmetric dihydroxylation as the key step in the enantioselective synthesis of spirocyclic σ1 receptor ligands. Tetrahedron Asymmetry 2014;25: 268–277. Abstract
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Junker A, Kokornaczyk AK, Strunz AK, Wünsch B. Selective and Dual Targeting of CCR2 and CCR5 Receptors: A Current Overview. Chemokines 2014: 1-55. Abstract
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Junker A, Schepmann D, Yamaguchi J, Itami K, Faust A, Kopka K, Wagner S, Wünsch B. Diverse modifications of the 4-methylphenyl moiety of TAK-779 by late-stage Suzuki-Miyaura cross-coupling. Org Biomol Chem 2014;12: 177-186. Abstract
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Miyata K, Moller G, Schepmann D, Wunsch B. Pyridine analogues of spirocyclic sigma(1) receptor ligands. Bioorg Med Chem 2014;22: 4277-4284. Abstract
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Miyata K, Schepmann D, Wunsch B. Synthesis and sigma receptor affinity of regioisomeric spirocyclic furopyridines. Eur J Med Chem 2014;83: 709-716. Abstract
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Schulte A, Saito S, Wünsch B. Stereoselective Synthesis of_cis_,_cis_-Configured Vicinal Triamines: Stereoselective Synthesis of_cis_,_cis_-Configured Vicinal Triamines. Eur J Org Chem 2014;2014: 5749-5756. Abstract
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Weber F, Brune S, Korpis K, Bednarski PJ, Laurini E, Dal Col V, Pricl S, Schepmann D, Wunsch B. Synthesis, pharmacological evaluation, and sigma1 receptor interaction analysis of hydroxyethyl substituted piperazines. J Med Chem 2014;57: 2884-2894. Abstract
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Brune S, Pricl S, Wunsch B. Structure of the sigma1 receptor and its ligand binding site. J Med Chem 2013;56: 9809-9819. Abstract
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Harel D, Schepmann D, Prinz H, Brun R, Schmidt TJ, Wunsch B. Natural product derived antiprotozoal agents: synthesis, biological evaluation, and structure-activity relationships of novel chromene and chromane derivatives. J Med Chem 2013;56: 7442-7448. Abstract
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Holl K, Falck E, Kohler J, Schepmann D, Humpf H-U, Brust P, Wunsch B. Synthesis, characterization, and metabolism studies of fluspidine enantiomers. ChemMedChem 2013;8: 2047-2056. Abstract
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Junker A, Yamaguchi J, Itami K, Wunsch B. Synthesis of thiophene-based TAK-779 analogues by C-H arylation. J Org Chem 2013;78: 5579-5586. Abstract
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Lueg C, Schepmann D, Gunther R, Brust P, Wunsch B. Development of fluorinated CB(2) receptor agonists for PET studies. Bioorg Med Chem 2013;21: 7481-7498. Abstract
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