期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 20, 期 22, 页码 6375-6378出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.09.098
关键词
T-type calcium channel; Ca(V)3.2; Diazaspirodecanones
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. (C) 2010 Elsevier Ltd. All rights reserved.
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