New azole antagonists with high affinity for the P2Y1 receptor

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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. © 2013 Elsevier Ltd. All rights reserved.

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Ruel, R., L’Heureux, A., Thibeault, C., Daris, J. P., Martel, A., Price, L. A., … Lam, P. Y. S. (2013). New azole antagonists with high affinity for the P2Y1 receptor. Bioorganic and Medicinal Chemistry Letters, 23(12), 3519–3522. https://doi.org/10.1016/j.bmcl.2013.04.041

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