From ATP to AZD6140: the discovery of an orally active reversible P2Y12 receptor antagonist for the prevention of thrombosis

Autor:	Anthony Ingall, Brian Springthorpe, Simon Guile, Chapman David, Paul D. Leeson, Timothy Nicholas Birkinshaw, Garry Pairaudeau, Simon F. Hunt, John Dixon, Michael Mortimore, Richard J. Lewis, Barry Teobald, Dermot F. McGinnity, Brown Roger Charles, Stuart W. Paine, Anil Patel, Robert J. Riley, Francis Ince, Wendy Tomlinson, Kirk Ian, Roger Bonnert, Andrew Bailey, Aaron Rigby, Patrick Barton, Paul Willis, Barrie Martin, P. Leff, R.G. Humphries, Peter J. H. Webborn
Rok vydání:	2007
Předmět:	Purine Ticagrelor Adenosine Clinical Biochemistry Pharmaceutical Science Administration Oral Pharmacology Biochemistry chemistry.chemical_compound Adenosine Triphosphate In vivo Oral administration Drug Discovery medicine Purinergic P2 Receptor Antagonists Animals Humans Receptor Molecular Biology Organic Chemistry Antagonist Membrane Proteins Thrombosis In vitro Receptors Purinergic P2Y12 chemistry Molecular Medicine Adenosine triphosphate medicine.drug
Zdroj:	Bioorganicmedicinal chemistry letters. 17(21)
ISSN:	0960-894X
Popis:	Starting from adenosine triphosphate (ATP), the identification of a novel series of P2Y(12) receptor antagonists and exploitation of their SAR is described. Modifications of the acidic side chain and the purine core and investigation of hydrophobic substituents led to a series of neutral molecules. The leading compound, 17 (AZD6140), is currently in a large phase III clinical trial for the treatment of acute coronary syndromes and prevention of thromboembolic clinical sequelae.
Databáze:	OpenAIRE
Externí odkaz:	https://explore.openaire.eu/search/publication?articleId=doi_dedup___::d6951535cd7d2c326d389158dd07fcea https://pubmed.ncbi.nlm.nih.gov/17827008 Zobrazit plný text záznamu Full Text from ScienceDirect