127033-39-0Relevant articles and documents
Synthesis and biological evaluation of novel quinazoline-4-piperidinesulfamide derivatives as inhibitors of NPP1
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
, p. 130 - 149 (2018/02/14)
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.