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

Autor:	C. David Weaver, Shuanghua Hu, Tracey Fiedler, Robert G. Gentles, Michael A. Poss, Katherine A. Grant-Young, Nicholas J. Lodge, C. J. Andres, David G. Harden, Ronald J. Knox, Yazhong Huang
Rok vydání:	2008
Předmět:	Stereochemistry Pyridines Small-Conductance Calcium-Activated Potassium Channels Clinical Biochemistry Pharmaceutical Science chemistry.chemical_element Calcium Apamin Biochemistry chemistry.chemical_compound Structure-Activity Relationship Drug Discovery medicine Potassium Channel Blockers Structure–activity relationship Combinatorial Chemistry Techniques Channel blocker Molecular Biology Molecular Structure Organic Chemistry Potassium channel blocker Potassium channel Electrophysiology Thiazoles chemistry Biophysics Molecular Medicine Thallium medicine.drug
Zdroj:	Bioorganicmedicinal chemistry letters. 18(19)
ISSN:	1464-3405
Popis:	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.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::7ad4d70227e7dcf6b1277c2291110a61 https://pubmed.ncbi.nlm.nih.gov/18774291 Zobrazit plný text záznamu Full Text from ScienceDirect