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New azole antagonists with high affinity for the P2Y1 receptor
Authors:Réjean Ruel  Alexandre L’Heureux  Carl Thibeault  Jean-Paul Daris  Alain Martel  Laura A. Price  Qimin Wu  Ji Hua  Ruth R. Wexler  Robert Rehfuss  Patrick Y.S. Lam
Affiliation:Research and Development, Bristol-Myers Squibb Company, Princeton, NJ 08543, USA
Abstract:Five-membered-ring heterocyclic urea mimics have been found to be potent and selective antagonists of the P2Y1 receptor. SAR of the various heterocyclic replacements is presented, as well as side-chain SAR of the more potent thiadiazole ring system which leads to thiadiazole 4c as a new antiplatelet agent.
Keywords:Purinergic receptor  Platelet aggregation  Five-membered-ring heterocyclic urea mimics  Thiadiazoles
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