This technology features a composition for inhibiting platelet aggregation, containing 2-((1H-indol-3-yl)methylene)-N-phenylhydrazinecarboxamide or its pharmaceutically acceptable salts, which possess a novel bioisostere scaffold. The same compound is formulated into pharmaceutical compositions for the prevention and treatment of thrombotic and cardiovascular diseases, as well as food compositions for their prevention and improvement.
Platelet aggregation is a primary cause of cardiovascular diseases such as stroke, coronary artery disease, and pulmonary embolism. Existing GPIIb/IIIa inhibitors directly compete with fibrinogen binding, leading to side effects like intracranial hemorrhage, retroperitoneal bleeding, and thrombocytopenia. Due to diagnostic uncertainty, many elderly patients are often unable to receive antiplatelet therapy, creating a need for effective and safer antiplatelet agents with new mechanisms of action.
Instead of directly blocking fibrinogen binding, this technology uses small-molecule compounds that target the GPIIb/IIIa activation step triggered by the interaction between the cytoskeletal protein talin and the GPIIIa tail to inhibit platelet aggregation. Target conditions include thrombotic diseases such as arterial and venous thrombosis, cerebral infarction, pulmonary infarction, and thrombophlebitis, as well as cardiovascular diseases such as hypertension, angina, myocardial infarction, atherosclerosis, and arrhythmia. It can be applied to acute coronary syndrome drug candidates, oral antithrombotic agents for preventing recurrent cerebral infarction, and health functional foods for blood circulation, offering a new antiplatelet treatment option that reduces the bleeding risks associated with existing GPIIb/IIIa antagonists.
This invention was developed with support from the Ministry of Science and ICT for the discovery and efficacy validation of novel antiplatelet agents targeting Glycoprotein IIb/IIIa inside-out signaling.
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