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 inhib...

Full description

Saved in:
Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2010-12, Vol.20 (23), p.6983-6988
Main Authors: Haffner, Curt D., Thomson, Stephen A., Guo, Yu, Schaller, Lee T., Boggs, Sharon, Dickerson, Scott, Gobel, Jeff, Gillie, Dan, Condreay, J. Patrick
Format: Article
Language:English
Subjects:
1,2-Benzothiazole
Amides
Animals
Benzamides - chemistry
Benzamides - pharmacology
Benzothiazoles - chemistry
Benzothiazoles - pharmacology
Biological and medical sciences
Cell Line
General and cellular metabolism. Vitamins
Humans
Kv1.3
Kv1.3 Potassium Channel - antagonists & inhibitors
Medical sciences
Pancreatitis-Associated Proteins
Patch-Clamp Techniques
Pharmacology. Drug treatments
Structure-Activity Relationship
Sulfonamides
Urea - analogs & derivatives
Voltage-gated potassium channel
Citations: Items that this one cites
Items that cite this one
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary: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. 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.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2010.09.132