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

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.
Curt D Haffner 1 Stephen A Thomson Yu Guo Lee T Schaller Sharon Boggs Scott Dickerson Jeff Gobel Dan Gillie J Patrick Condreay
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, GlaxoSmithKline Research and Development, Research Triangle Park, NC 27709, USA. curt.d.haffner@gsk.com
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.

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