Discovery of a novel series of selective HCN1 blockers

…, DH Lee, AD Wickenden, M Hermann, B Allison…

文献索引：McClure, Kelly J.; Maher, Michael; Wu, Nancy; Chaplan, Sandra R.; Eckert III, William A.; Lee, Dong H.; Wickenden, Alan D.; Hermann, Michelle; Allison, Brett; Hawryluk, Natalie; Breitenbucher, J. Guy; Grice, Cheryl A. Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 18 p. 5197 - 5201

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被引用次数: 15

摘要

The discovery of a series of novel, potent, and selective blockers of the cyclic nucleotide- modulated channel HCN1 is disclosed. Here we report an SAR study around a series of selective blockers of the HCN1 channel. Utilization of a high-throughput VIPR assay led to the identification of a novel series of 2, 2-disubstituted indane derivatives, which had moderate selectivity and potency at HCN1. Optimization of this hit led to the identification ...