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

Bioorganic & Medicinal Chemistry Letters
2008.0

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.

Knowledge Graph

Similar Paper

Initial SAR studies on apamin-displacing 2-aminothiazole blockers of calcium-activated small conductance potassium channels
Bioorganic & Medicinal Chemistry Letters 2008.0
Aminoalkynyldithianes. A new class of calcium channel blockers
Journal of Medicinal Chemistry 1991.0
Synthesis and SAR of 4-aminocyclopentapyrrolidines as N-type Ca2+ channel blockers with analgesic activity
Bioorganic & Medicinal Chemistry 2012.0
1,4,2-Benzo/pyridodithiazine 1,1-Dioxides Structurally Related to the ATP-Sensitive Potassium Channel Openers 1,2,4-Benzo/pyridothiadiazine 1,1-Dioxides Exert a Myorelaxant Activity Linked to a Distinct Mechanism of Action
Journal of Medicinal Chemistry 2013.0
Synthesis and Radioligand Binding Studies of Methoxylated 1,2,3,4-Tetrahydroisoquinolinium Derivatives as Ligands of the Apamin-Sensitive Ca<sup>2+</sup>-Activated K<sup>+</sup>Channels
Journal of Medicinal Chemistry 2006.0
Novel potent and selective Ca2+ release-activated Ca2+ (CRAC) channel inhibitors. Part 3: Synthesis and CRAC channel inhibitory activity of 4′-[(trifluoromethyl)pyrazol-1-yl]carboxanilides
Bioorganic &amp; Medicinal Chemistry 2008.0
Discovery of potent T-type calcium channel blocker
Bioorganic &amp; Medicinal Chemistry Letters 2007.0
Bis-tetrahydroisoquinoline derivatives: AG525E1, a new step in the search for non-quaternary non-peptidic small conductance Ca2+-activated K+ channel blockers
Bioorganic &amp; Medicinal Chemistry Letters 2008.0
The synthesis and structure–activity relationships of 3-amino-4-benzylquinolin-2-ones
Bioorganic &amp; Medicinal Chemistry Letters 2004.0
Synthesis and cytotoxic effects of 2-thio-3,4-dihydroquinazoline derivatives as novel T-type calcium channel blockers
Bioorganic &amp; Medicinal Chemistry 2020.0