Synthesis and SAR of pyrimidine-based, non-nucleotide P2Y14 receptor antagonists.

Journal Article (Journal Article)

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.

Full Text

Duke Authors

Cited Authors

  • 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

Published Date

  • May 2011

Published In

Volume / Issue

  • 21 / 10

Start / End Page

  • 2832 - 2835

PubMed ID

  • 21507642

Electronic International Standard Serial Number (EISSN)

  • 1464-3405

International Standard Serial Number (ISSN)

  • 0960-894X

Digital Object Identifier (DOI)

  • 10.1016/j.bmcl.2011.03.084


  • eng