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

  • Bioorg Med Chem Lett. 2010 Dec 1;20(23):6989-92. doi: 10.1016/j.bmcl.2010.09.131.
Curt D Haffner  1 ,  Stephen A Thomson ,  Yu Guo ,  Kimberly Petrov ,  Andrew Larkin ,  Pierette Banker ,  Gregory Schaaf ,  Scott Dickerson ,  Jeff Gobel ,  Dan Gillie ,  J Patrick Condreay ,  Chuck Poole ,  Tiffany Carpenter ,  John Ulrich
Affiliations
  • 1. Department of Medicinal Chemistry, GlaxoSmithKline Research and Development, Research Triangle Park, NC 27709, USA. [email protected]
PMID: 20974533 DOI: 10.1016/j.bmcl.2010.09.131
Abstract

We report the synthesis and in vitro activity of a series of novel substituted 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 demonstrated similar potency to the known Kv1.3 inhibitor PAP-1 when tested under the IonWorks patch clamp assay conditions. Two compounds 13i and 13rr were advanced further as potential tool compounds for in vivo validation studies.