Projects per year
In this perspective, coagulation factor XIIa (FXIIa), a serine protease implicated in the coagulation cascade, recently emerged as a promising target in the development of such agents2. Indeed, it was demonstrated that FXII deficiency or inhibition protects against thrombosis without causing spontaneous bleeding in mice3.
Based on these considerations, the aim of our project is to develop novel selective FXIIa inhibitors to detail the exact role of this enzyme in thrombotic diseases. These compounds could also be a good starting point for the development of new antithrombotic drugs.
The 3-carboxamide coumarins (figure 1) are to date the only nonpetidic and selective inhibitors of FXIIa described in literature4. However, their low solubility and poor pharmacokinetics resulted in a lack of activity in in vivo models of thrombosis. As consequence, we need to improve these characteristics while keeping the selectivity and potency towards FXIIa.
In this work, we first synthesized new coumarins with improved solubility. Their inhibition potency was then measured on FXIIa and finally, their stability was evaluated.
|Pages||Book of Abstracts, MedChem 2012, Château de Colonster, Liège - November 30, 2012, P01|
|Number of pages||1|
|Publication status||Published - 30 Nov 2012|
|Event||Annual One-Day Symposium on Medicinal Chemistry of SRC & KVCV (Medchem 2012) - Liège, Belgium|
Duration: 30 Nov 2012 → …
|Symposium||Annual One-Day Symposium on Medicinal Chemistry of SRC & KVCV (Medchem 2012)|
|Period||30/11/12 → …|
Eduard Dolusic (Contributor)30 Nov 2012
Activity: Participating in or organising an event types › Participation in conference
Conception, synthèse et évaluation biologique de coumarines en tant qu'inhibiteurs de protéases à sérineAuthor: Pochet, L., 2000
Supervisor: Masereel, B. (Supervisor)
Student thesis: Doc types › Doctor of Sciences
Supervisor: Durant, F. (Supervisor)
Student thesis: Master types › Master in Chemistry
Evaluation biologique de coumarines en tant qu'inhibiteurs de protéases à sérine de la cascade de la coagulationAuthor: Robert, S. H., 2004
Student thesis: Master types › Master in BiologyFile