Preliminary SAR studies on non-apamin-displacing 4-(aminomethylaryl)pyrrazolopyrimidine K(Ca) channel blockers |
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| Authors: | Gentles Robert G Hu Shuanghua Huang Yazhong Grant-Young Katherine Poss Michael A Andres Charles Fiedler Tracey Knox Ronald Lodge Nicholas Weaver C David Harden David G |
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| Affiliation: | Research and Development, Bristol Myers Squibb Co., 5 Research Parkway, Wallingford, CT, USA. robert.gentles@bms.com |
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| 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. |
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