Synthesis of Novel 3‐Butylphthalide Derivatives Containing Isopentenylphenol Moiety as Potential Antiplatelet Agents for the Treatment of Ischemic Stroke. Issue 1 (7th December 2022)

• Record Type: Journal Article
• Authors: Yu, Qinyang; Luo, Bilan; Luo, Zhongfu; Zhong, Xu; Li, Yi; Zhang, Yi; Zhu, Gaofeng; Guo, Bing; Tang, Lei; Li, Yong; Fan, Lingling
• Is Part Of: Chemistry & biodiversity. Volume 20:Issue 1(2023)
• Page Start: n/a
• Page End: n/a
• Publication Date: 2022-12-07
• Subjects: 3-butylphthalide derivatives -- antiplatelet activity -- antithrombotic activity -- cerebral ischemia reperfusion -- pharmacokinetic; Biochemistry -- Periodicals; Molecular biology -- Periodicals; Biodiversity -- Periodicals; 572
• DOI: 10.1002/cbdv.202201002
• Languages: English
• ISSNs: 1612-1872

Abstract

Abstract: In order to find novel antiplatelet drugs for the treatment of ischemic stroke, a series of 3‐butylphthalide derivatives containing isopentenylphenol moiety were designed, synthesized and characterized with spectroscopic analyses. The in vitro antiplatelet activity results indicated that compound 3 better inhibited the arachidonic acid (AA) induced platelet aggregation than aspirin (ASP) and 3‐butylphthalide (NBP). Additionally, compared with precursor NBP, compound 3 possessed outstanding antithrombotic activity in the animal experiment model, which could effectively alleviate the formation of tail thrombus and carotid artery thrombus in mice. More importantly, intraperitoneal administration of compound 3 can well protected the rats against ischemia/reperfusion‐induced brain injury. Further pharmacokinetic (PK) assay indicated that compound 3 had good absorption characteristics and metabolic stability in vivo . Overall, the present research provides a new candidate compound for the treatment of ischemic stroke caused by platelet aggregation. Abstract :