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ID: ALA1268989

Journal: Bioorg Med Chem Lett

Title: Design, syntheses, and SAR of 2,8-diazaspiro[4.5]decanones as T-type calcium channel antagonists.

Authors: Fritch PC, Krajewski J.

Abstract: It was hypothesized that an appropriately substituted 2,8-diazaspiro[4.5]decan-1-one could effectively approximate a 5-feature T-type pharmacophore model published in the literature. Compounds were designed and synthesized to test our hypothesis and were found to be potent T-type calcium channel inhibitors with modest selectivity over L-type calcium channels. The synthesis and SAR of the series is described.

CiteXplore: 20934333

DOI: 10.1016/j.bmcl.2010.09.098