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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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| Published in: | Bioorganic & medicinal chemistry letters 2008-12, Vol.18 (23), p.6222-6226 |
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| Main Authors: | , , , , , , , , , , , , , , , , |
| Format: | Article |
| Language: | English |
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| container_end_page | 6226 |
| container_issue | 23 |
| container_start_page | 6222 |
| container_title | Bioorganic & medicinal chemistry letters |
| container_volume | 18 |
| creator | 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 |
| description | 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. |
| doi_str_mv | 10.1016/j.bmcl.2008.09.102 |
| format | article |
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| fulltext | fulltext |
| identifier | EISSN: 1464-3405 |
| ispartof | Bioorganic & medicinal chemistry letters, 2008-12, Vol.18 (23), p.6222-6226 |
| issn | 1464-3405 |
| language | eng |
| recordid | cdi_proquest_miscellaneous_69773977 |
| source | Elsevier |
| 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 |
| title | Tetrahydro-4-quinolinamines identified as novel P2Y(1) receptor antagonists |
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