Thienopyrimidine-based P2Y12 platelet aggregation inhibitors.
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.
Kortum
Steven W
SW
Pfizer Global Research and Development, Pfizer Inc., St. Louis Laboratories, 700 Chesterfield Parkway West, Chesterfield, MO 63017, USA. steve.kortum@pfizer.com
Lachance
Rhonda M
RM
Schweitzer
Barbara A
BA
Yalamanchili
Gopichand
G
Rahman
Hayat
H
Ennis
Michael D
MD
Huff
Rita M
RM
TenBrink
Ruth E
RE
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
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