Literature DB >> 18774291

Initial SAR studies on apamin-displacing 2-aminothiazole blockers of calcium-activated small conductance potassium channels.

Robert G Gentles1, Katherine Grant-Young, Shuanghua Hu, Yazhong Huang, Michael A Poss, Charles Andres, Tracey Fiedler, Ronald Knox, Nicholas Lodge, C David Weaver, David G Harden.   

Abstract

An initial SAR study on a series of apamin-displacing 2-aminothiazole K(Ca)2 channel blockers is described. Potent inhibitors such as N-(4-methylpyridin-2-yl)-4-(pyridin-2-yl)thiazol-2-amine (13) are disclosed, and for select members of the series, the relationship between the observed activity in a thallium flux, a binding and a whole-cell electrophysiology assay is presented.

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Year:  2008        PMID： 18774291     DOI： 10.1016/j.bmcl.2008.08.023

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.823


  9 in total

1.  Pharmacological blockade of small conductance Ca2+-activated K+ channels by ICA reduces arrhythmic load in rats with acute myocardial infarction.

Authors:  Laura A Hundahl; Stefan M Sattler; Lasse Skibsbye; Jonas G Diness; Jacob Tfelt-Hansen; Thomas Jespersen
Journal:  Pflugers Arch       Date:  2017-03-11       Impact factor: 3.657

Review 2.  Small-molecule modulators of inward rectifier K+ channels: recent advances and future possibilities.

Authors:  Gautam Bhave; Daniel Lonergan; Brian A Chauder; Jerod S Denton
Journal:  Future Med Chem       Date:  2010-05       Impact factor: 3.808

Review 3.  Approaches for probing allosteric interactions at 7 transmembrane spanning receptors.

Authors:  Michael T Klein; Paige N Vinson; Colleen M Niswender
Journal:  Prog Mol Biol Transl Sci       Date:  2013       Impact factor: 3.622

Review 4.  Potassium currents in the heart: functional roles in repolarization, arrhythmia and therapeutics.

Authors:  Nipavan Chiamvimonvat; Ye Chen-Izu; Colleen E Clancy; Isabelle Deschenes; Dobromir Dobrev; Jordi Heijman; Leighton Izu; Zhilin Qu; Crystal M Ripplinger; Jamie I Vandenberg; James N Weiss; Gideon Koren; Tamas Banyasz; Eleonora Grandi; Michael C Sanguinetti; Donald M Bers; Jeanne M Nerbonne
Journal:  J Physiol       Date:  2017-01-05       Impact factor: 5.182

Review 5.  Small-conductance Ca2+ -activated K+ channels and cardiac arrhythmias.

Authors:  Xiao-Dong Zhang; Deborah K Lieu; Nipavan Chiamvimonvat
Journal:  Heart Rhythm       Date:  2015-05-05       Impact factor: 6.343

Review 6.  Cardiac small-conductance calcium-activated potassium channels in health and disease.

Authors:  Xiao-Dong Zhang; Phung N Thai; Deborah K Lieu; Nipavan Chiamvimonvat
Journal:  Pflugers Arch       Date:  2021-02-23       Impact factor: 3.657

7.  Suppression of AKT anti-apoptotic signaling by a novel drug candidate results in growth arrest and apoptosis of hepatocellular carcinoma cells.

Authors:  Andrea Cuconati; Courtney Mills; Cally Goddard; Xianchao Zhang; Wenquan Yu; Haitao Guo; Xiaodong Xu; Timothy M Block
Journal:  PLoS One       Date:  2013-01-23       Impact factor: 3.240

8.  Antiarrhythmic effect of the Ca2+-activated K+ (SK) channel inhibitor ICA combined with either amiodarone or dofetilide in an isolated heart model of atrial fibrillation.

Authors:  Jeppe Egedal Kirchhoff; Jonas Goldin Diness; Lea Abildgaard; Majid Sheykhzade; Morten Grunnet; Thomas Jespersen
Journal:  Pflugers Arch       Date:  2016-10-08       Impact factor: 3.657

9.  Small conductance calcium activated K+ channel inhibitor decreases stretch induced vulnerability to atrial fibrillation.

Authors:  Yannan Yan; Mark Alexander Skarsfeldt; Jonas Goldin Diness; Bo Hjorth Bentzen
Journal:  Int J Cardiol Heart Vasc       Date:  2021-10-23
  9 in total

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