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Bioorg Med Chem Lett. 2010 Jan 1;20(1):92-6. doi: 10.1016/j.bmcl.2009.11.029. Epub 2009 Nov 13.

Oxygenated analogues of UK-396082 as inhibitors of activated thrombin activatable fibrinolysis inhibitor.

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Pfizer Global Research and Development, Sandwich Laboratories, Ramsgate Road, Sandwich CT13 9NJ, UK.


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.

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