New azole antagonists with high affinity for the P2Y(1) receptor

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...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2013-06, Vol.23 (12), p.3519-3522
Main Authors: Ruel, Réjean, L'Heureux, Alexandre, Thibeault, Carl, Daris, Jean-Paul, Martel, Alain, Price, Laura A, Wu, Qimin, Hua, Ji, Wexler, Ruth R, Rehfuss, Robert, Lam, Patrick Y S
Format: Article
Language:English
Subjects:
Biomimetic Materials - chemistry
Biomimetic Materials - pharmacology
Humans
Kinetics
Protein Binding
Purinergic P2Y Receptor Antagonists - chemistry
Purinergic P2Y Receptor Antagonists - pharmacology
Receptors, Purinergic P2Y1 - chemistry
Structure-Activity Relationship
Thiadiazoles - chemistry
Thiadiazoles - pharmacology
Urea - chemistry
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Summary: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.
ISSN:1464-3405
DOI:10.1016/j.bmcl.2013.04.041