1.
Bioorg Med Chem Lett
; 20(14): 4104-7, 2010 Jul 15.
Article
in English
| MEDLINE
| ID: mdl-20542694
ABSTRACT
Benzofuran-substituted urea analogs have been identified as novel P2Y(1) receptor antagonists. Structure-activity relationship studies around the urea and the benzofuran moieties resulted in compounds having improved potency. Several analogs were shown to inhibit ADP-mediated platelet activation.
Subject(s)
Benzofurans/chemistry , Purinergic P2Y Receptor Antagonists/chemistry , Receptors, Purinergic P2Y1/metabolism , Urea/chemistry , Benzofurans/pharmacology , Platelet Activation/drug effects , Purinergic P2Y Receptor Antagonists/pharmacology , Urea/pharmacology
2.
Bioorg Med Chem Lett
; 18(23): 6222-6, 2008 Dec 01.
Article
in English
| MEDLINE
| ID: mdl-18926700
ABSTRACT
High-throughput screening of the GSK compound collection against the P2Y(1) receptor identified a novel series of tetrahydro-4-quinolinamine antagonists. Optimal substitution around the piperidine group was pivotal for ensuring activity. An exemplar analog from this series was shown to inhibit platelet aggregation.
