Tetrahydro-4-quinolinamines identified as novel P2Y(1) receptor antagonists

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 plate...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2008-12, Vol.18 (23), p.6222-6226
Main Authors: Morales-Ramos, Angel I, Mecom, John S, Kiesow, Terry J, Graybill, Todd L, Brown, Gregory D, Aiyar, Nambi V, Davenport, Elizabeth A, Kallal, Lorena A, Knapp-Reed, Beth A, Li, Peng, Londregan, Allyn T, Morrow, Dwight M, Senadhi, Shobha, Thalji, Reema K, Zhao, Steve, Burns-Kurtis, Cynthia L, Marino, Jr, Joseph P
Format: Article
Language:English
Subjects:
Aminoquinolines - chemical synthesis
Aminoquinolines - chemistry
Aminoquinolines - pharmacology
Combinatorial Chemistry Techniques
Humans
Molecular Structure
Platelet Aggregation Inhibitors - chemical synthesis
Platelet Aggregation Inhibitors - chemistry
Platelet Aggregation Inhibitors - pharmacology
Purinergic P2 Receptor Antagonists
Receptors, Purinergic P2 - metabolism
Receptors, Purinergic P2Y1
Stereoisomerism
Structure-Activity Relationship
Thrombosis - drug therapy
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Summary: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.
ISSN:1464-3405
DOI:10.1016/j.bmcl.2008.09.102