title: Thienopyrimidine-based P2Y12 platelet aggregation inhibitors.
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.
authors.affiliation: Pfizer Global Research and Development, Pfizer Inc., St. Louis Laboratories, 700 Chesterfield Parkway West, Chesterfield, MO 63017, USA. steve.kortum@pfizer.com
authors.forename: Steven W
authors.initials: SW
authors.lastname: Kortum
authors.forename: Rhonda M
authors.initials: RM
authors.lastname: Lachance
authors.forename: Barbara A
authors.initials: BA
authors.lastname: Schweitzer
authors.forename: Gopichand
authors.initials: G
authors.lastname: Yalamanchili
authors.forename: Hayat
authors.initials: H
authors.lastname: Rahman
authors.forename: Michael D
authors.initials: MD
authors.lastname: Ennis
authors.forename: Rita M
authors.initials: RM
authors.lastname: Huff
authors.forename: Ruth E
authors.initials: RE
authors.lastname: TenBrink
mesh_terms: D005343:Fibrinolytic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D006801:Humans; D010974:Platelet Aggregation / Q000187:drug effects*; D010975:Platelet Aggregation Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D011485:Protein Binding; D058919:Purinergic P2 Receptor Antagonists; D011743:Pyrimidines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D018048:Receptors, Purinergic P2 / Q000378:metabolism; D058925:Receptors, Purinergic P2Y12; D013329:Structure-Activity Relationship
chemical_list: D005343:Fibrinolytic Agents; C548576:P2RY12 protein, human; D010975:Platelet Aggregation Inhibitors; D058919:Purinergic P2 Receptor Antagonists; D011743:Pyrimidines; D018048:Receptors, Purinergic P2; D058925:Receptors, Purinergic P2Y12; C476003:thienopyrimidine