Calcific aortic valve disease (CAVD) is the most common heart valve disorder in the United States and Western Europe. Thus far, there is no pharmaceutical treatment to prevent the mineralization of aortic valves, only valve replacement when illness patient is far advanced.1 Recent studies have shown that an increase of expression and enzymatic activity of ectonucleotide pyrophosphatase/phosphodiesterase 1 (ENPP1) promotes the mineralization process of the aortic valve. In this context, ENPP1 inhibition represents a major challenge. Herein, we will describe the synthesis of two categories of potential inhibitors in addition to their in vitro activity.2 (1) Mathieu, P. et al. J. Mol. Cell. Cardiol. 2012, 52, 1191-1202. (2) Shayhidin, E. E.; Forcellini, E.; Boulanger, M.-C.; Mahmut, A.; Dautrey, S.; Barbeau, X.; Lagüe, P.; Sévigny, J.; Paquin, J.-F.; Mathieu, P. Br. J. Pharmacol. 2015, 172, 4189-4199.

Synthesis and in vitro activity of ectonucleotide pyrophosphatase / phosphodiesterase 1 inhibitors

251st National Meeting (2016)

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