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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

✍ Scribed by Curt D. Haffner; 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

Book ID: 104004962
Publisher: Elsevier Science
Year: 2010
Tongue: English
Weight: 335 KB
Volume: 20
Category: Article
ISSN: 0960-894X
DOI: 10.1016/j.bmcl.2010.09.131

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✦ Synopsis

a b s t r a c t

We report the synthesis and in vitro activity of a series of novel substituted N-{3-[(1,1-dioxido-1,2benzothiazol-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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