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Can I read Pharmacophore-based search, synthesis, and biological evaluation of anthranilic amides as novel blockers of the Kv1.5 channel on EtoBox?
Pharmacophore-based search, synthesis, and biological evaluation of anthranilic amides as novel blockers of the Kv1.5 channel by Stefan Peukert; Joachim Brendel; Bernard Pirard; Carsten Strübing; Heinz-Werner Kleemann; Thomas Böhme; Horst Hemmerle is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.
What is Pharmacophore-based search, synthesis, and biological evaluation of anthranilic amides as novel blockers of the Kv1.5 channel about?
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.
Who reads Pharmacophore-based search, synthesis, and biological evaluation of anthranilic amides as novel blockers of the Kv1.5 channel?
It is typically read by researchers, students, and practitioners in Biochemistry, Genetics and Molecular Biology.
- Author
- Stefan Peukert; Joachim Brendel; Bernard Pirard; Carsten Strübing; Heinz-Werner Kleemann; Thomas Böhme; Horst Hemmerle
- Publisher
- Elsevier Science; Elsevier ; Elsevier Ltd.; Elsevier BV (ISSN 0960-894X)
- Published
- 2004
- Language
- EN
- Field
- Biochemistry, Genetics and Molecular Biology (Life Sciences)