Design and synthesis of macrocyclic indoles targeting blood coagulation cascade Factor XIa

The synthesis of a series of novel macrocyclic compounds designed to target blood coagulation Factor XIa is described. The compounds were evaluated for their inhibition of a small set of serine proteases. Several compounds displayed modest activity and good selectivity for Factor XIa. Within the ser...

Ausführliche Beschreibung

Gespeichert in:

Bibliographische Detailangaben
Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2010-12, Vol.20 (23), p.6925-6928
Hauptverfasser:	Hanessian, Stephen, Larsson, Andreas, Fex, Tomas, Knecht, Wolfgang, Blomberg, Niklas
Format:	Artikel
Sprache:	eng
Schlagworte:	Anticoagulants - chemical synthesis Anticoagulants - pharmacology Biological and medical sciences Blood Coagulation - drug effects Blood. Blood coagulation. Reticuloendothelial system Drug Design Enzyme inhibitor Factor XIa - antagonists & inhibitors Indoles - chemistry Indoles - pharmacology Macrocycle Medical sciences Pharmacology. Drug treatments Serine Proteinase Inhibitors - chemistry Serine Proteinase Inhibitors - pharmacology Structure-Activity Relationship Thrombin
Online-Zugang:	Volltext
Tags:	Tag hinzufügen Keine Tags, Fügen Sie den ersten Tag hinzu!

Beschreibung
Zusammenfassung:	The synthesis of a series of novel macrocyclic compounds designed to target blood coagulation Factor XIa is described. The compounds were evaluated for their inhibition of a small set of serine proteases. Several compounds displayed modest activity and good selectivity for Factor XIa. Within the series, a promising lead structure for developing novel macrocyclic inhibitors of thrombin was identified.
ISSN:	0960-894X 1464-3405 1464-3405
DOI:	10.1016/j.bmcl.2010.09.141