Pyrrolidine amides of pyrazolodihydropyrimidines as potent and selective Kv1.5 blockers

Design and synthesis of pyrazolodihydropyrimidines as KV1.5 blockers led to the discovery of 7d as a potent and selective antagonist. This compound showed atrial selective prolongation of effective refractory period in rabbits and was selected for clinical development.

Gespeichert in:

Bibliographische Detailangaben
Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2010-02, Vol.20 (4), p.1436-1439
Hauptverfasser:	LLOYD, John, FINLAY, Heather J, HONG SHI, HUANG, Christine, DANSHI LI, HUABIN SUN, LEVESQUE, Paul, VACARRO, Wayne, HYUNH, Tram, KOVER, Alexander, BHANDARU, Rao, LIN YAN, ATWAL, Karnail, LEE CONDER, Mary, JENKINS-WEST, Tonya
Format:	Artikel
Sprache:	eng
Schlagworte:	Amides - chemical synthesis Amides - chemistry Amides - pharmacology Animals Antiarythmic agents Biological and medical sciences Cardiovascular system Dogs Dose-Response Relationship, Drug Inhibitory Concentration 50 Kv1.5 Potassium Channel - antagonists & inhibitors Medical sciences Molecular Structure Pharmacology. Drug treatments Potassium Channel Blockers - chemical synthesis Potassium Channel Blockers - chemistry Potassium Channel Blockers - pharmacology Pyrazoles - pharmacology Pyrrolidines - chemical synthesis Pyrrolidines - chemistry Pyrrolidines - pharmacology Rabbits Rats
Online-Zugang:	Volltext
Tags:	Tag hinzufügen Keine Tags, Fügen Sie den ersten Tag hinzu!

Beschreibung
Zusammenfassung:	Design and synthesis of pyrazolodihydropyrimidines as KV1.5 blockers led to the discovery of 7d as a potent and selective antagonist. This compound showed atrial selective prolongation of effective refractory period in rabbits and was selected for clinical development.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2009.12.085