N-{3-[(1,1-dioxido-1,2-benzothiazol-3-yl)(phenyl)amino]propyl}benzamide analogs as potent Kv1.3 inhibitors. Part 1

Bioorg Med Chem Lett. 2010 Dec 1;20(23):6983-8. doi: 10.1016/j.bmcl.2010.09.132. Epub 2010 Oct 7.

Abstract

We report the synthesis and in vitro activity of a series of novel N-{3-[(1,1-dioxido-1,2-benzothiazol-3-yl)(phenyl)amino]propyl}benzamide analogs. These analogs showed potent inhibitory activity against Kv1.3. Several compounds, including compound 8b, showed similar potency to the known Kv1.3 inhibitor PAP-1 when tested under the IonWorks patch clamp assay conditions.

MeSH terms

  • Amides
  • Animals
  • Benzamides / chemistry*
  • Benzamides / pharmacology
  • Benzothiazoles / chemistry*
  • Benzothiazoles / pharmacology
  • Cell Line
  • Humans
  • Kv1.3 Potassium Channel / antagonists & inhibitors*
  • Pancreatitis-Associated Proteins
  • Patch-Clamp Techniques
  • Structure-Activity Relationship
  • Sulfonamides
  • Urea / analogs & derivatives

Substances

  • Amides
  • Benzamides
  • Benzothiazoles
  • Kv1.3 Potassium Channel
  • Pancreatitis-Associated Proteins
  • REG3A protein, human
  • Sulfonamides
  • Urea