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Updated: Jun 6, 2025

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Published on: September 5, 2016
Design and Synthesis of Butylphthalide-Hydroxycinnamic Acid Hybrid Derivatives as Potential Antiplatelet Agents
Ya Yang1, Zhen Jia1, Taigui Ma1
1College of Pharmacy, Guizhou Provincial Engineering Technology Research Center for Chemical Drug R&D, Guizhou Provincial Key Laboratory of Pathogenesis and Drug Research on Common Chronic Diseases, Guizhou Medical University, Guiyang, 550004, People's Republic of China.
Abstract:
Thirty-eight novel butylphthalide-hydroxycinnamic acid hybrid derivatives were designed and synthesized to discover effective antiplatelet agglutination drugs. Among these compounds, 3 o gave the optimal inhibitory activity against AA-induced platelet aggregation in vitro and also exhibited better inhibition than the precursor 3-n-butylphthalide (NBP) against thrombin-induced platelet contraction, carrageenan-induced tail thrombosis, and FeCl3-induced common carotid artery thrombosis. Further investigations on the anti-ischemic stroke activity revealed that compound 3 o exhibited a remarkable protective effect against ischemic/reperfusion brain injury. The PAMPA-BBB permeability and liver microsomal stability tests indicated that compound 3 o could traverse the blood-brain barrier and possessed favorable metabolic stability. This research provides a new candidate compound for treating and preventing cerebrovascular diseases caused by thrombosis.
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