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Bioorg Med Chem Lett. 2006 Nov 15;16(22):5897-901. Epub 2006 Sep 1.

Potent antagonists of the Kv1.5 potassium channel: synthesis and evaluation of analogous N,N-diisopropyl-2-(pyridine-3-yl)acetamides.

Author information

1
Department of Medicinal Chemistry, Merck Research Laboratories, Merck and Co., Inc., PO Box 4, West Point, PA 19486, USA.

Abstract

This letter describes the discovery of a novel series of potent Kv1.5 ion channel antagonists based on a diisopropyl amide scaffold. Structure-activity relationships of functionalized analogs are discussed. Key compound 1-(3-(diisopropylcarbamoyl)-2-phenyl-3-(pyridin-3-yl)propyl)-3-(2-fluorobenzyl)urea (10) exhibits significant atrial-selective effects in an in vivo model.

PMID:
16949818
DOI:
10.1016/j.bmcl.2006.08.054
[Indexed for MEDLINE]

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