Výsledky vyhledávání - "Eric Wellner"

Identification of novel GPR81 agonist lead series for target biology evaluation

Autor: Kristina Berggren, Nils-Olov Hermansson, Petra Johannesson, Annika Wellner, Jonas Brånalt, Kristina Nilsson, Henrik Gradén, Maria Ölwegård-Halvarsson, Ola Fjellström, Bengt Ohlsson, Terese Andersson, Öjvind Davidsson, Linda Gustafsson, Christian Tyrchan, Yantao Chen, Frank Jansen, Eric Wellner

Publikováno v: Bioorganicmedicinal chemistry letters. 30(4)

GPR81 is a novel drug target that is implicated in the control of glucose and lipid metabolism. The lack of potent GPR81 modulators suitable for in vivo studies has limited the pharmacological characterization of this lactate sensing receptor. We per

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::539ac9eaa5f8cfea396b0726436c5a3b
https://pubmed.ncbi.nlm.nih.gov/31932225

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Can Silicon Make an Excellent Drug Even Better? An in vitro and in vivo Head-to-Head Comparison between Loperamide and Its Silicon Analogue Sila-Loperamide

Autor: Duncan Armstrong, Eric Wellner, Marcel Geyer, Sebastian Saloman, Reinhold Tacke, Ulrik Jurva

Publikováno v: ChemMedChem. 10:911-924

Loperamide (1a), an opioid receptor agonist, is in clinical use as an antidiarrheal agent. Carbon/silicon exchange (sila-substitution) at the 4-position of the piperidine ring of 1a (R3 COH→R3 SiOH) leads to sila-loperamide (1b). Sila-loperamide wa

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c688d0be65bcb97e7ff655ea114bf94f
https://doi.org/10.1002/cmdc.201500040

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GPR103 Antagonists Demonstrating Anorexigenic Activity in Vivo: Design and Development of Pyrrolo[2,3-c]pyridines That Mimic the C-Terminal Arg-Phe Motif of QRFP26

Autor: Dorota Kakol-Palm, Eric Wellner, Henriksson Anette Marie Svensson, Martin J Watson, Zhong-Qing Yuan, Udo Bauer, Charles D. Blundell, Magnus Johansson, Yiqun Zhou, Lisbeth Kristensson, Anneli Nordqvist, Christian Tyrchan, Peter Brodin, Jennie Georgsson, Fredrik Bergström, Annika U. Petersson

Publikováno v: Journal of Medicinal Chemistry. 57:5935-5948

GPR103, a G-protein coupled receptor, has been reported to have orexigenic properties through activation by the endogenous neuropeptide ligands QRFP26 and QRFP43. Recognizing that central administration of QRFP26 and QRFP43 increases high fat food in

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::643c7da5be2aa635024058971f7d892c
https://doi.org/10.1021/jm401951t

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Synthesis and photophysical characterisation of new fluorescent triazole adenine analogues

Autor: Eric Wellner, Morten Grøtli, Anke Dierckx, Christopher P. Lawson, Francois-Alexandre Miannay, L. Marcus Wilhelmsson

Publikováno v: Org. Biomol. Chem.. 12:5158-5167

Fluorescent nucleic acid base analogues are powerful probes of DNA structure. Here we describe the synthesis and photo-physical characterisation of a series of 2-(4-amino-5-(1H-1,2,3-triazol-4-yl)-7H-pyrrolo[2,3-d]pyrimidin-7-yl) and 2-(4-amino-3-(1H

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b14edc4d870a386ee4f7f6d806067c16
https://doi.org/10.1039/c4ob00904e

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Sila-Haloperidol, a Silicon Analogue of the Dopamine (D2) Receptor Antagonist Haloperidol: Synthesis, Pharmacological Properties, and Metabolic Fate

Autor: Reinhold Tacke, Friedrich Popp, Matthias U. Kassack, Eric Wellner, Alexandra Hamacher, Dirk Schepmann, Christian Burschka, Barbara Müller, Ulrik Jurva, Bastian Theis, Bernhard Wünsch

Publikováno v: ChemMedChem. 3:152-164

Haloperidol (1 a), a dopamine (D(2)) receptor antagonist, is in clinical use as an antipsychotic agent. Carbon/silicon exchange (sila-substitution) at the 4-position of the piperidine ring of 1 a (R(3)COH --> R(3)SiOH) leads to sila-haloperidol (1 b)

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::53458d16b6a99ef02d87bd4b25a6568c
https://doi.org/10.1002/cmdc.200700205

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Synthesis and Pharmacological Properties of Silicon-Containing GPR81 and GPR109A Agonists

Autor: Reinhold Tacke, Marcel Geyer, Eric Wellner, Ola Fjellström, Linda Gustafsson, Johannes A. Baus

Publikováno v: ChemMedChem. 10(12)

The GPR81 and GPR109A receptors mediate antilipolytic effects and are potential drug targets for the treatment of metabolic disorders such as dyslipidemia and type 2 diabetes. There is still a need to identify potent GPR81 agonists as pharmacological

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::db399b4b1a318fbda0cc2b880fe45329
https://pubmed.ncbi.nlm.nih.gov/26459194

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Si- and C-Functional Organosilicon Building Blocks for Synthesis Based on 4-Silacyclohexan-1-ones Containing the Silicon Protecting Groups MOP (4-Methoxyphenyl), DMOP (2,6-Dimethoxyphenyl), or TMOP (2,4,6-Trimethoxyphenyl)

Autor: Johannes A. Baus, Reinhold Tacke, Marcel Geyer, Olle Karlsson, Eric Wellner

Publikováno v: The Journal of organic chemistry. 80(11)

4-Silacyclohexan-1-ones 1a–1c, 4-silacyclohexan-1-one oximes 2a–2c, 1,4-azasilepan-7-ones 3a–3c, 1,4-azasilepanes 4a–4c, and 2-bromo-4-silacyclohexan-1-ones 5a and 5b were prepared in multistep syntheses, starting from trimethoxypropylsilane.

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::b2c43a1512030ab45592d6dadc66042e
https://pubmed.ncbi.nlm.nih.gov/25928726

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A Fast and Parallel Route to Cyclic Isothioureas and Guanidines with Use of Microwave-Assisted Chemistry

Autor: Marie-Louise Swanstein, Eric Wellner, Helena Sandin

Publikováno v: The Journal of Organic Chemistry. 69:1571-1580

A fast and simple approach to novel cyclic isothioureas and related guanidine derivatives is presented in this study. The construction of the central basic scaffolds is achieved solely by the application of microwave-assisted chemistry, without any n

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::2d01020ecf528ef05f3de19b0ad2d816
https://doi.org/10.1021/jo030338m

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