A novel series of piperazinyl-pyridine ureas as antagonists of the purinergic P2Y12 receptor

Peter Bach; Jonas Boström; Kay Brickmann; J J J van Giezen; Ragnar Hovland; Annika U Petersson; Asim Ray; Fredrik Zetterberg

doi:10.1016/j.bmcl.2011.03.088

A novel series of piperazinyl-pyridine ureas as antagonists of the purinergic P2Y12 receptor

Bioorg Med Chem Lett. 2011 May 15;21(10):2877-81. doi: 10.1016/j.bmcl.2011.03.088. Epub 2011 Mar 30.

Authors

Peter Bach¹, Jonas Boström, Kay Brickmann, J J J van Giezen, Ragnar Hovland, Annika U Petersson, Asim Ray, Fredrik Zetterberg

Affiliation

¹ Department of Medicinal Chemistry, AstraZeneca R&D, Pepparedsleden 1, S-43183 Mölndal, Sweden. Peter.Bach@astrazeneca.com

PMID: 21507636
DOI: 10.1016/j.bmcl.2011.03.088

Abstract

A novel series of P2Y(12) antagonists for development of drugs within the antiplatelet area is presented. The synthesis of the piperazinyl-pyridine urea derivatives and their structure-activity relationships (SAR) are described. Several compounds showed P2Y(12) antagonistic activities in the sub-micromolar range.

MeSH terms

Inhibitory Concentration 50
Molecular Structure
Piperazines / chemistry*
Platelet Aggregation Inhibitors / chemical synthesis
Platelet Aggregation Inhibitors / pharmacology
Protein Binding / drug effects
Purinergic Antagonists / chemical synthesis*
Purinergic Antagonists / chemistry
Purinergic Antagonists / pharmacology*
Pyridines / chemistry*
Receptors, Purinergic P2Y12 / metabolism
Structure-Activity Relationship
Urea / chemical synthesis*
Urea / chemistry
Urea / pharmacology*

Substances

Piperazines
Platelet Aggregation Inhibitors
Purinergic Antagonists
Pyridines
Receptors, Purinergic P2Y12
Urea