Stereoselective Synthesis of New (2S,3R)-3-Carboxyphenyl)pyrrolidine-2-carboxylic Acid Analogues Utilizing a C(sp3)–H Activation Strategy and Structure–Activity Relationship Studies at the Ionotropic Glutamate Receptors

Autor: Jacob C. Hansen, Silke Kayser, Kasper B. Hansen, Stylianos Iliadis, Niels Krogsgaard-Larsen, Lennart Bunch, Darryl S. Pickering, Jed T. Syrenne, Markus Staudt, Piero Temperini, Younes Larsen, Birgitte Nielsen, Feng Yi, Aleksandra Moroz

Publikováno v: ACS Chemical Neuroscience. 11:674-701

Competitive antagonists for ionotropic glutamate receptors (iGluRs) are highly valuable tool compounds for studying health and disease states in the central nervous system. However, only few subtype selective tool compounds are available and the disc

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::b74894f5acdfe0a342e18b7b5c2a7a0e
https://doi.org/10.1021/acschemneuro.0c00003

Augmentation of Anticancer Drug Efficacy in Murine Hepatocellular Carcinoma Cells by a Peripherally Acting Competitive N-Methyl-d-aspartate (NMDA) Receptor Antagonist

Autor: Seppo Auriola, Kasper B. Hansen, Mikko Gynther, Yevheniia Ishchenko, Darryl S. Pickering, Birgitte Nielsen, Aleksanteri Petsalo, Younes Larsen, Liwei Han, Jacob C. Hansen, Silke Kayser, Ilaria Proietti Silvestri, Tarja Malm, Lennart Bunch

Publikováno v: Journal of Medicinal Chemistry. 60:9885-9904

The most common solid tumors show intrinsic multidrug resistance (MDR) or inevitably acquire suchwhen treated with anticancer drugs. In this work, we describe the discovery of a peripherally restricted, potent, competitive NMDA receptor antagonist 1l

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2d18f06ffb40ecf3c324f127febf63d4
https://doi.org/10.1021/acs.jmedchem.7b01624

Synthesis of a Dual-Purpose 2-Deoxy-2-fluoro-glucopyranosyl Building Block

Autor: Jacob C. Hansen, Henrik H. Jensen, Anja B. Christiansen, Agnete H. Viuff

Publikováno v: Viuff, A H, Hansen, J C, Christiansen, A B & Jensen, H H 2013, ' Synthesis of a dual-purpose 2-deoxy-2-fluoro-glucopyranosyl building block ', Synthetic Communications, vol. 43, no. 11, pp. 1557-1562 . https://doi.org/10.1080/00397911.2011.648001

We demonstrate a straightforward route to 1,3,6-tri-O-acetyl-4-O-benzyl-2-deoxy-2-fluoro-D-glucopyranose through potassium hydrogen fluoride opening of a Cerný epoxide under microwave irradiation followed by acetolysis. The fluoroglucose building bl

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::8a991ce42ce2ecc69dd22b9e7688a666
https://doi.org/10.1080/00397911.2011.648001

Identification of a New Class of Selective Excitatory Amino Acid Transporter Subtype 1 (EAAT1) Inhibitors Followed by a Structure-Activity Relationship Study

Autor: Walden E. Bjørn-Yoshimoto, Anders A. Jensen, Stinne W. Hansen, Lennart Bunch, Jacob C. Hansen, Bjarke Abrahamsen, Bingru Fu, Mette N. Erichsen

Publikováno v: Journal of medicinal chemistry. 59(19)

Screening of a small compound library at the three excitatory amino acid transporter subtypes 1-3 (EAAT1-3) resulted in the identification of compound (Z)-4-chloro-3-(5-((3-(2-ethoxy-2-oxoethyl)-2,4-dioxothiazolidin-5-ylidene)methyl)furan-2-yl)benzoi

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::399df88bc78016dff3140765282e6162
https://pubmed.ncbi.nlm.nih.gov/27626828

Convenient access to β-substituted cysteines and β- and γ-mercapto prolines.

Autor: Hansen, Jacob C., Rabuffetti, Marco, Bunch, Lennart LeBu@sund.ku.dk

Publikováno v: Canadian Journal of Chemistry. May2023, Vol. 101 Issue 5, p326-333. 8p.