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Your search keyword '"Roine I"' showing total 6 results
Start Over Author "Roine I" Publisher elsevier b.v.
6 results on '"Roine I"'

1. Lactam sulfonamides as potent inhibitors of the Kv1.5 potassium ion channel.

Author

Olsson, Roine I., Jacobson, Ingemar, Iliefski, Tommy, Boström, Jonas, Davidsson, Öjvind, Fjellström, Ola, Björe, Annika, Olsson, Christina, Sundell, Johan, Gran, Ulrik, Gyll, Jonna, Malmberg, Jesper, Hidestål, Olle, Emtenäs, Hans, Svensson, Tor, Yuan, Zhong-Qing, Strandlund, Gert, Åstrand, Annika, Lindhardt, Emma, and Linhardt, Gunilla

Subjects
*SULFONAMIDES, *LACTAMS, *POTASSIUM channels, *IN vitro studies, *STRUCTURE-activity relationships, *MOLECULAR structure, *ATRIAL fibrillation treatment
Abstract

Abstract: A series of lactam sulfonamides has been discovered and optimized as inhibitors of the Kv1.5 potassium ion channel for treatment of atrial fibrillation. In vitro structure–activity relationships from lead structure C to optimized structure 3y are described. Compound 3y was evaluated in a rabbit PD-model and was found to selectively prolong the atrial effective refractory period at submicromolar concentrations. [Copyright &y& Elsevier]

Published
2014
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2. Synthesis and evaluation of diphenylphosphinic amides and diphenylphosphine oxides as inhibitors of Kv1.5

Author

Olsson, Roine I., Jacobson, Ingemar, Boström, Jonas, Fex, Tomas, Björe, Annika, Olsson, Christina, Sundell, Johan, Gran, Ulrik, Öhrn, Anna, Nordin, Andreas, Gyll, Jonna, Thorstensson, Maria, Hayen, Ahlke, Aplander, Karolina, Hidestål, Olle, Jiang, Fanyi, Linhardt, Gunilla, Forsström, Elin, Collins, Teresa, and Sundqvist, Monika

Subjects
*AMIDE synthesis, *DIPHENYLPHOSPHINE, *POTASSIUM channels, *ATRIAL fibrillation treatment, *STRUCTURE-activity relationships, *LABORATORY rabbits
Abstract

Abstract: Diphenylphosphinic amides and diphenylphosphine oxides have been synthesized and tested as inhibitors of the Kv1.5 potassium ion channel as a possible treatment for atrial fibrillation. In vitro structure–activity relationships are discussed and several compounds with Kv1.5 IC50 values of <0.5μM were discovered. Selectivity over the ventricular IKs current was monitored and selective compounds were found. Results from a rabbit PD-model are included. [Copyright &y& Elsevier]

Published
2013
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4. Novel thioamide derivatives as neutral CB1 receptor antagonists

Author

Boström, Jonas, Olsson, Roine I., Tholander, Joakim, Greasley, Peter J., Ryberg, Erik, Nordberg, Henrik, Hjorth, Stephan, and Cheng, Leifeng

Subjects
*AMIDES, *CANNABINOIDS, *DRUG receptors, *OBESITY treatment, *BODY weight, *PYRAZINES, *LABORATORY mice, *CHEMICAL inhibitors, *THERAPEUTICS
Abstract

Abstract: A novel class of cannabinoid-1 (CB1) receptor antagonists for the treatment of obesity is presented. The carboxamide linker in a set of 5,6-diaryl-pyrazine-2-amide derivatives was transformed into the corresponding thioamide, by using a one-pot synthesis. The structural series of thioamides not only showed retained CB1 potency (below 10nM), but also showed improved solubility. In addition, the neutral antagonist 2c significantly reduced body weight in cafeteria diet obese mice. [Copyright &y& Elsevier]

Published
2010
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6. Isoindolinone compounds active as Kv1.5 blockers identified using a multicomponent reaction approach.

Author

Kajanus, Johan, Jacobson, Ingemar, Åstrand, Annika, Olsson, Roine I., Gran, Ulrik, Björe, Annika, Fjellström, Ola, Davidsson, Öjvind, Emtenäs, Hans, Dahlén, Anders, Löfberg, Boel, Yuan, Zhong-Qing, Sundell, Johan, Cassel, Johan, Gyll, Jonna, Iliefski, Tommy, Högberg, Ågot, Lindhardt, Emma, and Malmberg, Jesper

Subjects
*INDOLINONE, *POTASSIUM antagonists, *STRUCTURE-activity relationship in pharmacology, *MEAN volume rate (Chemistry), *PARTITION coefficient (Chemistry)
Abstract

A series of isoindolinone compounds have been developed showing good in vitro potency on the Kv1.5 ion channel. By modification of two side chains on the isoindolinone scaffold, metabolically stable compounds with good in vivo PK profile could be obtained leaving the core structure unsubstituted. In this way, low microsomal intrinsic clearance (CLint) could be achieved despite a relatively high logD. The compounds were synthesized using the Ugi reaction, in some cases followed by Suzuki and Diels–Alder reactions, giving a diverse set of compounds in a small number of reaction steps. [ABSTRACT FROM AUTHOR]

Published
2016
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