Why the study?
Do novel carba-nucleosides antagonize the P2Y12 receptor and inhibit human platelet aggregation?
Do novel carba-nucleosides antagonize the P2Y12 receptor and inhibit human platelet aggregation?
Novel carba-nucleoside tetrazole derivatives demonstrate high-affinity P2Y12 receptor antagonism and potent inhibition of human platelet aggregation in vitro.
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Hypothesis-generating for tetrazole-based P2Y12 antagonists; does not support clinical translation without further validation.
Antagonizing a key platelet purinergic receptor. The wide clinical use of clopidogrel has highlighted the importance of platelet ADP receptor (P2Y12) antagonists for preventing adverse cardiovascular events. We synthesized a series of novel carba-nucleosides and examined their usefulness as P2Y12 antagonists. Some tetrazole derivatives were high-affinity receptor antagonists and potent inhibitors of human platelet aggregation.
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Hong et al. (2008) studied this question.
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