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Publikationer i urvalet

20 träffar

Bibliografisk träff 2019-10-08

Impact of hydroxy moieties at the benzo[7]annulene ring system of GluN2B ligands: Design, synthesis and biological evaluation.

Temme L, Börgel F, Schepmann D, Robaa D, Sippl W, Daniliuc C, Wünsch B.

Bioorg Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmc.2019.115146

Bibliografisk träff 2019-06-20

Modification of the 4-phenylbutyl side chain of potent 3-benzazepine-based GluN2B receptor antagonists.

Wagner M, Schepmann D, Ametamey SM, Wünsch B.

Bioorg Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmc.2019.06.035

Bibliografisk träff 2019-05-16

Tetrahydro-3-benzazepines with fluorinated side chains as NMDA and σ<sub>1</sub> receptor antagonists: Synthesis, receptor affinity, selectivity and antiallodynic activity.

Thum S, Schepmann D, Ayet E, Pujol M, Nieto FR, Ametamey SM, Wünsch B.

Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2019.05.034

Bibliografisk träff 2017-12-18

Hydroxymethyl bioisosteres of phenolic GluN2B-selective NMDA receptor antagonists: Design, synthesis and pharmacological evaluation.

Temme L, Frehland B, Schepmann D, Robaa D, Sippl W, Wünsch B.

Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2017.12.054

Bibliografisk träff 2017-12-07

2-Methyltetrahydro-3-benzazepin-1-ols - The missing link in SAR of GluN2B selective NMDA receptor antagonists.

Dey S, Schepmann D, Wünsch B.

Bioorg Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmc.2017.12.010

Bibliografisk träff 2017-07-29

Replacement of benzylic hydroxy group by vinyl or hydroxymethyl moiety at the 3-benzazepine scaffold retaining GluN2B affinity.

Rath S, Schepmann D, Wünsch B.

Bioorg Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmc.2017.07.059

Bibliografisk träff 2017-07-01

Deconstruction - reconstruction approach to analyze the essential structural elements of tetrahydro-3-benzazepine-based antagonists of GluN2B subunit containing NMDA receptors.

Dey S, Temme L, Schreiber JA, Schepmann D, Frehland B, Lehmkuhl K, Strutz-Seebohm N, Seebohm G, Wünsch B.

Eur J Med Chem · journal article · DOI 10.1016/j.ejmech.2017.06.068

Bibliografisk träff 2017-03-17

Do GluN2B subunit containing NMDA receptors tolerate a fluorine atom in the phenylalkyl side chain?

Shuto Y, Thum S, Temme L, Schepmann D, Kitamura M, Wünsch B.

Medchemcomm · research-article; journal article · DOI 10.1039/c6md00621c

Bibliografisk träff 2015-12-21

Role of the phenolic OH moiety of GluN2B-selective NMDA antagonists with 3-benzazepine scaffold.

Dey S, Schepmann D, Wünsch B.

Bioorg Med Chem Lett · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmcl.2015.12.067

Bibliografisk träff 2015-10-31

Benzo[7]annulene-based GluN2B selective NMDA receptor antagonists: Surprising effect of a nitro group in 2-position.

Gawaskar S, Schepmann D, Bonifazi A, Robaa D, Sippl W, Wünsch B.

Bioorg Med Chem Lett · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmcl.2015.10.076

Bibliografisk träff 2015-10-14

Novel Potent N-Methyl-d-aspartate (NMDA) Receptor Antagonists or σ1 Receptor Ligands Based on Properly Substituted 1,4-Dioxane Ring.

Bonifazi A, Del Bello F, Mammoli V, Piergentili A, Petrelli R, Cimarelli C, Pellei M, Schepmann D, Wünsch B, Barocelli E, Bertoni S, Flammini L, Amantini C, Nabissi M, Santoni G, Vistoli G, Quaglia W.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/acs.jmedchem.5b01214

Bibliografisk träff 2014-10-12

Synthesis, GluN2B affinity and selectivity of benzo[7]annulen-7-amines.

Gawaskar S, Schepmann D, Bonifazi A, Wünsch B.

Bioorg Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmc.2014.10.004

Bibliografisk träff 2014-08-05

Synthesis and pharmacological evaluation of 5-pyrrolidinylquinoxalines as a novel class of peripherally restricted κ-opioid receptor agonists.

Bourgeois C, Werfel E, Galla F, Lehmkuhl K, Torres-Gómez H, Schepmann D, Kögel B, Christoph T, Straßburger W, Englberger W, Soeberdt M, Hüwel S, Galla HJ, Wünsch B.

J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1021/jm500940q

Bibliografisk träff 2012-10-09

Enantiomerically pure 1,3-dioxanes as highly selective NMDA and σ₁ receptor ligands.

Köhler J, Bergander K, Fabian J, Schepmann D, Wünsch B.

J Med Chem · journal article · DOI 10.1021/jm301166m

Bibliografisk träff 2011-03-05

Synthesis of 4-(aminoalkyl) substituted 1,3-dioxanes as potent NMDA and σ receptor antagonists.

Utech T, Köhler J, Wünsch B.

Eur J Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.ejmech.2011.02.070

Bibliografisk träff 2010-09-25

Synthesis and SAR studies of chiral non-racemic dexoxadrol analogues as uncompetitive NMDA receptor antagonists.

Banerjee A, Schepmann D, Köhler J, Würthwein EU, Wünsch B.

Bioorg Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmc.2010.09.047

Bibliografisk träff 2010-09-24

Conformationally constrained NR2B selective NMDA receptor antagonists derived from ifenprodil: Synthesis and biological evaluation of tetrahydro-3-benzazepine-1,7-diols.

Tewes B, Frehland B, Schepmann D, Schmidtke KU, Winckler T, Wünsch B.

Bioorg Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmc.2010.09.026

Bibliografisk träff 2010-04-04

Synthesis and NMDA receptor affinity of fluorinated dioxadrol analogues.

Banerjee A, Schepmann D, Wünsch B.

Bioorg Med Chem · research support, non-u.s. gov't; journal article · DOI 10.1016/j.bmc.2010.04.002

Bibliografisk träff 1992-04-01

Analogues of the dioxolanes dexoxadrol and etoxadrol as potential phencyclidine-like agents. Synthesis and structure-activity relationships.

Thurkauf A, Mattson MV, Richardson S, Mirsadeghi S, Ornstein PL, Harrison EA, Rice KC, Jacobson AE, Monn JA.

J Med Chem · research support, u.s. gov't, p.h.s.; research support, non-u.s. gov't; journal article · DOI 10.1021/jm00086a001

Bibliografisk träff 1988-12-01

Synthesis, absolute configuration, and molecular modeling study of etoxadrol, a potent phencyclidine-like agonist.

Thurkauf A, Zenk PC, Balster RL, May EL, George C, Carroll FI, Mascarella SW, Rice KC, Jacobson AE, Mattson MV.

J Med Chem · research support, u.s. gov't, p.h.s.; research support, non-u.s. gov't; journal article · DOI 10.1021/jm00120a004