PubMed 25801931

Referenced in Channelpedia wiki pages of: none

Automatically associated channels: Kv1.5

Title: Pseudosaccharin amines as potent and selective KV1.5 blockers.

Authors: John Lloyd, Heather J Finlay, Alexander Kover, James Johnson, Zulan Pi, Ji Jiang, James Neels, Cullen Cavallaro, Ruth Wexler, Mary Lee Conder, Hong Shi, Danshi Li, Huabin Sun, Anjaneya Chimalakonda, Christine Huang, Mark Salvati, Paul Levesque

Journal, date & volume: Bioorg. Med. Chem. Lett., 2015 Mar 7 , ,

PubMed link:

Phenethyl aminoheterocycles like compound 1 were known to be potent I(Kur) blockers although they lacked potency in vivo. Modification of the heterocycle led to the design and synthesis of pseudosaccharin amines. Compounds such as 14, 17d and 21c were found to be potent K(V)1.5 blockers and selective over other cardiac ion channels. These compounds had potent pharmacodynamic activity, however, they also showed off-target activities such as hemodynamic effects.