- Preliminary SAR studies on non-apamin-displacing 4-(aminomethylaryl)pyrrazolopyrimidine K(Ca) channel blockers.
Preliminary SAR studies on non-apamin-displacing 4-(aminomethylaryl)pyrrazolopyrimidine K(Ca) channel blockers.
Bioorganic & medicinal chemistry letters (2008-10-01)
Robert G Gentles, Shuanghua Hu, Yazhong Huang, Katherine Grant-Young, Michael A Poss, Charles Andres, Tracey Fiedler, Ronald Knox, Nicholas Lodge, C David Weaver, David G Harden
PMID18824351
ABSTRACT
An exploratory SAR study on a series of potent, non-apamin-displacing 4-(aminomethylaryl)pyrazolopyrimidine K(Ca) channel blockers is described and their selectivity against K(Ca) channel subtypes is reported. The most potent analog, 5-chloro-N-(thiophen-2-ylmethyl)pyrazolo[1,5-a]pyrimidin-7-amine (24) displayed sub-micromolar activity in both a thallium flux and whole-cell electrophysiology assay and did not displace apamin in a competitive binding study.