New azole antagonists with high affinity for the P2Y(1) receptor

Réjean Ruel; Alexandre L'Heureux; Carl Thibeault; Jean-Paul Daris; Alain Martel; Laura A Price; Qimin Wu; Ji Hua; Ruth R Wexler; Robert Rehfuss; Patrick Y S Lam

doi:10.1016/j.bmcl.2013.04.041

New azole antagonists with high affinity for the P2Y(1) receptor

Bioorg Med Chem Lett. 2013 Jun 15;23(12):3519-22. doi: 10.1016/j.bmcl.2013.04.041. Epub 2013 Apr 25.

Authors

Réjean Ruel¹, Alexandre L'Heureux, Carl Thibeault, Jean-Paul Daris, Alain Martel, Laura A Price, Qimin Wu, Ji Hua, Ruth R Wexler, Robert Rehfuss, Patrick Y S Lam

Affiliation

¹ Research and Development, Bristol-Myers Squibb Company, Princeton, NJ 08543, USA. [email protected]

PMID: 23668989
DOI: 10.1016/j.bmcl.2013.04.041

Abstract

Five-membered-ring heterocyclic urea mimics have been found to be potent and selective antagonists of the P2Y1 receptor. SAR of the various heterocyclic replacements is presented, as well as side-chain SAR of the more potent thiadiazole ring system which leads to thiadiazole 4c as a new antiplatelet agent.

Publication types

Letter

MeSH terms

Biomimetic Materials / chemistry
Biomimetic Materials / pharmacology
Humans
Kinetics
Protein Binding
Purinergic P2Y Receptor Antagonists / chemistry*
Purinergic P2Y Receptor Antagonists / pharmacology*
Receptors, Purinergic P2Y1 / chemistry*
Structure-Activity Relationship
Thiadiazoles / chemistry*
Thiadiazoles / pharmacology*
Urea / chemistry

Substances

Purinergic P2Y Receptor Antagonists
Receptors, Purinergic P2Y1
Thiadiazoles
Urea