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 |
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| Authors: | Haffner Curt D Thomson Stephen A Guo Yu Petrov Kimberly Larkin Andrew Banker Pierette Schaaf Gregory Dickerson Scott Gobel Jeff Gillie Dan Condreay J Patrick Poole Chuck Carpenter Tiffany Ulrich John |
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| Institution: | Department of Medicinal Chemistry, GlaxoSmithKline Research and Development, Research Triangle Park, NC 27709, USA. curt.d.haffner@gsk.com |
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| 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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