Skip to main page content
U.S. flag

An official website of the United States government

Dot gov

The .gov means it’s official.
Federal government websites often end in .gov or .mil. Before sharing sensitive information, make sure you’re on a federal government site.

Https

The site is secure.
The https:// ensures that you are connecting to the official website and that any information you provide is encrypted and transmitted securely.

Access keys NCBI Homepage MyNCBI Homepage Main Content Main Navigation
. 2007 Nov 1;17(21):6013-8.
doi: 10.1016/j.bmcl.2007.07.057. Epub 2007 Aug 19.

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

Brian Springthorpe  1 , 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
Affiliations

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

Brian Springthorpe et al. Bioorg Med Chem Lett. .

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.

PubMed Disclaimer

MeSH terms

LinkOut - more resources