N-{3-[(1,1-dioxido-1,2-benzothiazol-3-yl)(phenyl)amino]propyl}benzamide analogs as potent Kv1.3 inhibitors. Part 1.
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.
Department of Medicinal Chemistry, GlaxoSmithKline Research and Development, Research Triangle Park, NC 27709, USA. curt.d.haffner@gsk.com
Curt D
CD
Haffner
Stephen A
SA
Thomson
Yu
Y
Guo
Lee T
LT
Schaller
Sharon
S
Boggs
Scott
S
Dickerson
Jeff
J
Gobel
Dan
D
Gillie
J Patrick
JP
Condreay
D000577:Amides; D000818:Animals; D001549:Benzamides / Q000737:chemistry* / Q000494:pharmacology; D052160:Benzothiazoles / Q000737:chemistry* / Q000494:pharmacology; D002460:Cell Line; D006801:Humans; D051664:Kv1.3 Potassium Channel / Q000037:antagonists & inhibitors*; D000073718:Pancreatitis-Associated Proteins; D018408:Patch-Clamp Techniques; D013329:Structure-Activity Relationship; D013449:Sulfonamides; D014508:Urea / Q000031:analogs & derivatives
D000577:Amides; D001549:Benzamides; D052160:Benzothiazoles; D051664:Kv1.3 Potassium Channel; D000073718:Pancreatitis-Associated Proteins; C000612141:REG3A protein, human; D013449:Sulfonamides; D014508:Urea