European Journal of Medicinal Chemistry p. 130 - 149 (2018)
Update date:2022-08-16
Topics:
Forcellini, Elsa
Boutin, Sophie
Lefebvre, Carole-Anne
Shayhidin, Elnur Elyar
Boulanger, Marie-Chloé
Rhéaume, Gabrielle
Barbeau, Xavier
Lagüe, Patrick
Mathieu, Patrick
Paquin, Jean-Fran?ois
The ecto-nucleotide pyrophosphatase/phosphodiesterase-1 (NPP1) was recently shown to promote mineralization of the aortic valve, hence, its inhibition represents a significant target. A quinazoline-4-piperidine sulfamide compound (QPS1) has been described as a specific and non-competitive inhibitor of NPP1. We report herein the synthesis and in vitro inhibition studies of novel quinazoline-4-piperidine sulfamide analogues using QPS1 as the lead compound. Of the 26 derivatives prepared, four compounds were found to have Ki < 105 nM against human NPP1.
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