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

Research output: Contribution to journalArticle

Abstract

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.

Details

Authors
External organisations
  • AstraZeneca, Sweden
Research areas and keywords

Keywords

  • Anticoagulants/chemical synthesis, Blood Coagulation/drug effects, Drug Design, Factor XIa/antagonists & inhibitors, Indoles/chemistry, Serine Proteinase Inhibitors/chemistry, Structure-Activity Relationship
Original languageEnglish
Pages (from-to)6925-6928
JournalBioorganic & Medicinal Chemistry Letters
Volume20
Issue number23
Publication statusPublished - 2010 Dec 1
Publication categoryResearch
Peer-reviewedYes
Externally publishedYes