1.
Bioorg Med Chem Lett
; 19(20): 5919-23, 2009 Oct 15.
Article
in English
| MEDLINE
| ID: mdl-19748783
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.
Subject(s)
Fibrinolytic Agents/chemistry , Platelet Aggregation Inhibitors/chemistry , Platelet Aggregation/drug effects , Purinergic P2 Receptor Antagonists , Pyrimidines/chemistry , Fibrinolytic Agents/chemical synthesis , Fibrinolytic Agents/pharmacology , Humans , Platelet Aggregation Inhibitors/chemical synthesis , Platelet Aggregation Inhibitors/pharmacology , Protein Binding , Pyrimidines/chemical synthesis , Pyrimidines/pharmacology , Receptors, Purinergic P2/metabolism , Receptors, Purinergic P2Y12 , Structure-Activity Relationship
2.
Bioorg Med Chem Lett
; 17(12): 3378-83, 2007 Jun 15.
Article
in English
| MEDLINE
| ID: mdl-17434734
ABSTRACT
The design and synthesis of a novel series of potent BACE1 hydroxyethylamine inhibitors. These inhibitors feature hydrogen bonding substituents at the C-5 position of the isophthalamide ring with improved selectivity over cathepsin D.