2. Academic Validation
  3. 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

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

Affiliation

  • 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.

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