Compound 9-2p demonstrated significant antiplatelet activity with IC50 values of 41.7 and 22.2 μM (ADP and thrombin) and GPIIb/IIIa antagonistic activity (IC50 2.3 μM).
Do novel 1,4-benzodioxine derivatives inhibit platelet aggregation and exhibit antithrombotic activity?
Compound 9-2p is a novel 1,4-benzodioxine derivative demonstrating moderate antiplatelet and antithrombotic activity via GPIIb/IIIa antagonism, serving as a potential lead for further drug optimization.
Aim: To find novel platelet aggregation inhibitors, two new series of 1,4-benzodioxine derivatives were synthesized and screened for the ability to inhibit platelet aggregation. Materials & methods: The synthesized compounds were evaluated for antiplatelet aggregation activity using human blood platelet and GPIIb/IIIa antagonistic activity. Results: Compound 9-2p showed significant antiplatelet activity with the IC50 values of 41.7 and 22.2 μM induced by ADP and thrombin, respectively, more potent than that of LX2421. Compound 9-2p exhibited GPIIb/IIIa antagonistic activity with the IC50 value of 2.3 μM, as potent as RGDs. In vivo study showed that 9-2p displayed remarkable antithrombotic activity, more effective than LX2421, but less effective than tirofiban. Conclusion: Compound 9-2p showed moderate antiplatelet activity and antithrombotic activity, which could be further optimized based on the target of GPIIb/IIIa.
Xie et al. (Tue,) conducted a other in Platelet aggregation / Thrombosis. Compound 9-2p (1,4-benzodioxine derivative) vs. LX2421, RGDs, and tirofiban was evaluated on Antiplatelet aggregation activity and GPIIb/IIIa antagonistic activity (IC50). Compound 9-2p demonstrated significant antiplatelet activity with IC50 values of 41.7 and 22.2 μM (ADP and thrombin) and GPIIb/IIIa antagonistic activity (IC50 2.3 μM).
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