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pubmed-article:15125940pubmed:abstractTextThe 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.lld:pubmed
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pubmed-article:15125940pubmed:articleTitlePharmacophore-based search, synthesis, and biological evaluation of anthranilic amides as novel blockers of the Kv1.5 channel.lld:pubmed
pubmed-article:15125940pubmed:affiliationAventis Pharma Deutschland GmbH, Medicinal Chemistry and DG Cardiovascular, D-65926 Frankfurt, Germany. stefan.peukert@aventis.comlld:pubmed
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