570398-47-9Relevant academic research and scientific papers
Oxygenated analogues of UK-396082 as inhibitors of activated thrombin activatable fibrinolysis inhibitor
Owen, Dafydd R.,Bull, David J.,Bunnage, Mark E.,Glossop, Melanie S.,Maguire, Robert J.,Strang, Ross S.
scheme or table, p. 92 - 96 (2010/04/24)
A suitable inhibitor of activated thrombin activatable fibrinolysis inhibitor (TAFIa) has the potential to be a novel treatment for thrombosis. The TAFIa inhibitor UK-396082 (1) was used as a starting point to seek more potent analogues. With knowledge of encouraging human pharmacokinetics and toleration for the clinical candidate (1), the programme continued to seek structure-activity relationships (SAR) that could positively impact on both potency and half-life, and therefore the projected dose of any future nominated clinical agent. A series of oxygenated analogues based on compound 1 were prepared to evaluate changes in pharmacology, selectivity and pharmacokinetics.
