Výsledky vyhledávání - "Thomas Antonsson"

Discovery of AZD4831, a Mechanism-Based Irreversible Inhibitor of Myeloperoxidase, As a Potential Treatment for Heart Failure with Preserved Ejection Fraction

Autor: Tord Inghardt, Thomas Antonsson, Cecilia Ericsson, Daniel Hovdal, Petra Johannesson, Carina Johansson, Ulrik Jurva, Johan Kajanus, Bengt Kull, Erik Michaëlsson, Anna Pettersen, Tove Sjögren, Henrik Sörensen, Kristina Westerlund, Eva-Lotte Lindstedt

Publikováno v: Journal of Medicinal Chemistry. 65:11485-11496

Myeloperoxidase is a promising therapeutic target for treatment of patients suffering from heart failure with preserved ejection fraction (HFpEF). We aimed to discover a covalent myeloperoxidase inhibitor with high selectivity for myeloperoxidase ove

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::97ef1bcb1b44e92cc2a14d39e9d3d4b8
https://doi.org/10.1021/acs.jmedchem.1c02141

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Potassium channel blocking 1,2-bis(aryl)ethane-1,2-diamines active as antiarrhythmic agents

Autor: Johan Kajanus, Leif Carlsson, Thomas Antonsson, Anna Pettersen, Johan Sundell, Tord Inghardt, Ulrik Jurva

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 29:1241-1245

Atrial fibrillation (AF) is a major cause of stroke, heart failure, sudden death and cardiovascular morbidity. The Kv1.5 potassium channel conducts the IKur current and has been demonstrated to be predominantly expressed in atrial versus ventricular

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::ed757dd1104a6385cd41b2c629e7f3db
https://doi.org/10.1016/j.bmcl.2019.03.006

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Iridium‐Catalyzed Asymmetric Hydrogenation of N ‐Alkyl α‐Aryl Furan‐Containing Imines: an Efficient Route to Unnatural N ‐Alkyl Arylalanines and Related Derivatives

Autor: Javier Mazuela, Rachel H. Munday, Magnus Johansson, Stephen P. Marsden, Thomas Antonsson, Laurent Knerr

Publikováno v: Advanced Synthesis & Catalysis. 361:578-584

High throughput experimentation (HTE) has enabled the rapid identification of ligand/precatalyst combinations that facilitate highly enantioselective hydrogenations of prochiral N‐alkyl α‐aryl ketimines containing a furyl moiety. The chiral amin

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_________::e1899a66b44e0b3aa212692a2de279f5
https://doi.org/10.1002/adsc.201801143

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Direct Synthesis of N-Alkyl Arylglycines by Organocatalytic Asymmetric Transfer Hydrogenation of N-Alkyl Aryl Imino Esters

Autor: Thomas Antonsson, Laurent Knerr, Stephen P. Marsden, Magnus Johansson, Javier Mazuela

Publikováno v: Organic Letters. 19:5541-5544

The organocatalytic asymmetric transfer hydrogenation of N-alkyl aryl imino esters for the direct synthesis of N-alkylated arylglycinate esters is reported. High yields and enantiomeric ratios were obtained, and tolerance to a diverse set of function

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::43d0e5a64e7b4525f85a8f3acdde9f0b
https://doi.org/10.1021/acs.orglett.7b02627

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Structural and functional characterization of a specific antidote for ticagrelor

Autor: Linda Öster, Sven Nylander, Mark Austin, Philip Newton, Peter Gennemark, Thomas Antonsson, Tord Inghardt, Annika Janefeldt, Andrew Buchanan, Jennifer Spooner, Feenagh Keyes, Garnet E. Howells, Ann-Sofie Sandinge, Mark Penney, Susanne Pehrsson, Tristan J. Vaughan, Peder Svensson, Tove Sjögren

Publikováno v: Blood. 125:3484-3490

Ticagrelor is a direct-acting reversibly binding P2Y12 antagonist and is widely used as an antiplatelet therapy for the prevention of cardiovascular events in acute coronary syndrome patients. However, antiplatelet therapy can be associated with an i

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::54ccab1e24a8a81600a0aceb00ead5bf
https://doi.org/10.1182/blood-2015-01-622928

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Optimization of ketone-based P2Y12 receptor antagonists as antithrombotic agents: Pharmacodynamics and receptor kinetics considerations

Autor: Lotta Hideståhl, David Brown, Ruth Bylund, Fabrizio Giordanetto, Helen Zachrisson, Jan-Arne Björkman, Fredrik Zetterberg, Daniel Hovdal, Peter Bach, Mikael Sellen, Thomas Antonsson, Pia Berntsson, Johan Johansson, J.J.J. van Giezen

Publikováno v: Bioorganic & Medicinal Chemistry Letters. 24:2963-2968

Modification of a series of P2Y12 receptor antagonists by replacement of the ester functionality was aimed at minimizing the risk of in vivo metabolic instability and pharmacokinetic variability. The resulting ketones were then optimized for their P2

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::c5ed48b479fe7b50a6ccea0af9931c04
https://doi.org/10.1016/j.bmcl.2014.04.001

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Lead Optimization of Ethyl 6-Aminonicotinate Acyl Sulfonamides as Antagonists of the P2Y12 Receptor. Separation of the Antithrombotic Effect and Bleeding for Candidate Drug AZD1283

Autor: Ruth Bylund, Jan-Arne Björkman, J.J.J. van Giezen, Thomas Antonsson, Fabrizio Giordanetto, Søren M. Andersen, Fredrik Zetterberg, Krister Österlund, Peter Bach, Helen Zachrisson

Publikováno v: Journal of Medicinal Chemistry. 56:7015-7024

Synthesis and structure-activity relationships of ethyl 6-aminonicotinate acyl sulfonamides, which are potent antagonists of the P2Y12 receptor, are presented. Shifting from 5-chlorothienyl to benzyl sulfonamides significantly increased the potency i

Externí odkaz: https://explore.openaire.eu/search/publication?articleId=doi_dedup___::f6bf90454944693e2720d14dccde13db
https://doi.org/10.1021/jm400820m

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