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

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}b enzamide analogs. These analogs showed potent inhibitory activity against Kv1.3. Several demonstrated similar potency to the known Kv1.3 inhibitor PAP-1 when...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2010-12, Vol.20 (23), p.6989-6992
Main Authors: Haffner, Curt D, Thomson, Stephen A, Guo, Yu, Petrov, Kimberly, Larkin, Andrew, Banker, Pierette, Schaaf, Gregory, Dickerson, Scott, Gobel, Jeff, Gillie, Dan, Condreay, JPatrick, Poole, Chuck, Carpenter, Tiffany, Ulrich, John
Format: Article
Language:English
Subjects:
Ion channels
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Summary: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}b enzamide 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.
ISSN:0960-894X
DOI:10.1016/j.bmcl.2010.09.131