Publications [#330220] of Michael J. Therien

Papers Published

1. Guay, D; Beaulieu, C; Belley, M; Crane, SN; DeLuca, J; Gareau, Y; Hamel, M; Henault, M; Hyjazie, H; Kargman, S; Chan, CC; Xu, L; Gordon, R; Li, L; Mamane, Y; Morin, N; Mancini, J; Thérien, M; Tranmer, G; Truong, VL; Wang, Z; Black, WC, Synthesis and SAR of pyrimidine-based, non-nucleotide P2Y14 receptor antagonists., Bioorganic & medicinal chemistry letters, vol. 21 no. 10 (May, 2011), pp. 2832-2835 [doi]
   (last updated on 2026/01/14)

   Abstract:
   A weak antagonist of the pyrimidinergic receptor P2Y(14) containing a dihydropyridopyrimidine core was identified through high-throughput screening. Subsequent optimization led to potent, non-UTP competitive antagonists and represent the first reported non-nucleotide antagonists of this receptor. Compound 18q was identified as a 10 nM P2Y(14) antagonist with good oral bioavailability and provided sufficient exposure in mice to be used as a tool for future in vivo studies.