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...

Ausführliche Beschreibung

Gespeichert in:

Bibliographische Detailangaben
Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2010-12, Vol.20 (23), p.6983-6988
Hauptverfasser:	Haffner, Curt D., Thomson, Stephen A., Guo, Yu, Schaller, Lee T., Boggs, Sharon, Dickerson, Scott, Gobel, Jeff, Gillie, Dan, Condreay, J. Patrick
Format:	Artikel
Sprache:	eng
Schlagworte:	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
Online-Zugang:	Volltext
Tags:	Tag hinzufügen Keine Tags, Fügen Sie den ersten Tag hinzu!

Beschreibung
Zusammenfassung:	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