Thienopyrimidine-based P2Y12 platelet aggregation inhibitors

Steven W Kortum; Rhonda M Lachance; Barbara A Schweitzer; Gopichand Yalamanchili; Hayat Rahman; Michael D Ennis; Rita M Huff; Ruth E TenBrink

doi:10.1016/j.bmcl.2009.08.059

Thienopyrimidine-based P2Y12 platelet aggregation inhibitors

Bioorg Med Chem Lett. 2009 Oct 15;19(20):5919-23. doi: 10.1016/j.bmcl.2009.08.059. Epub 2009 Aug 20.

Authors

Steven W Kortum¹, Rhonda M Lachance, Barbara A Schweitzer, Gopichand Yalamanchili, Hayat Rahman, Michael D Ennis, Rita M Huff, Ruth E TenBrink

Affiliation

¹ Pfizer Global Research and Development, Pfizer Inc., St. Louis Laboratories, 700 Chesterfield Parkway West, Chesterfield, MO 63017, USA. steve.kortum@pfizer.com

PMID: 19748783
DOI: 10.1016/j.bmcl.2009.08.059

Abstract

Herein we describe the design and synthesis of a novel series of potent thienopyrimidine P2Y12 inhibitors and the negative impact protein binding has on the inhibition of platelet aggregation.

MeSH terms

Fibrinolytic Agents / chemical synthesis
Fibrinolytic Agents / chemistry*
Fibrinolytic Agents / pharmacology
Humans
Platelet Aggregation / drug effects*
Platelet Aggregation Inhibitors / chemical synthesis
Platelet Aggregation Inhibitors / chemistry*
Platelet Aggregation Inhibitors / pharmacology
Protein Binding
Purinergic P2 Receptor Antagonists*
Pyrimidines / chemical synthesis
Pyrimidines / chemistry*
Pyrimidines / pharmacology
Receptors, Purinergic P2 / metabolism
Receptors, Purinergic P2Y12
Structure-Activity Relationship

Substances

Fibrinolytic Agents
P2RY12 protein, human
Platelet Aggregation Inhibitors
Purinergic P2 Receptor Antagonists
Pyrimidines
Receptors, Purinergic P2
Receptors, Purinergic P2Y12
thienopyrimidine