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ID: ALA1148261
Journal: Bioorg Med Chem Lett
Title: Pharmacophore-based search, synthesis, and biological evaluation of anthranilic amides as novel blockers of the Kv1.5 channel.
Authors: Peukert S, Brendel J, Pirard B, Strübing C, Kleemann HW, Böhme T, Hemmerle H.
Abstract: The search for novel, potent Kv1.5 blockers based on an anthranilic amide scaffold employing a pharmacophore-based virtual screening approach is described. The synthesis and structure-activity relationships (SAR) with respect to inhibition of the Kv1.5 channel are discussed. The most potent compounds display sub-micromolar inhibition of Kv1.5 and no significant effect on the HERG channel. In addition, good oral bioavailability is demonstrated for compound 3i in rats.
CiteXplore: 15125940