| Literature DB >> 17827008 |
Brian Springthorpe1, Andrew Bailey, Patrick Barton, Timothy N Birkinshaw, Roger V Bonnert, Roger C Brown, David Chapman, John Dixon, Simon D Guile, Robert G Humphries, Simon F Hunt, Francis Ince, Anthony H Ingall, Ian P Kirk, Paul D Leeson, Paul Leff, Richard J Lewis, Barrie P Martin, Dermot F McGinnity, Michael P Mortimore, Stuart W Paine, Garry Pairaudeau, Anil Patel, Aaron J Rigby, Robert J Riley, Barry J Teobald, Wendy Tomlinson, Peter J H Webborn, Paul A Willis.
Abstract
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.Entities:
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Year: 2007 PMID： 17827008 DOI： 10.1016/j.bmcl.2007.07.057
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823