1078720-35-0Relevant academic research and scientific papers
Design and synthesis of the ring-opened derivative of 3-n-butylphthalide-ferulic acid-glucose trihybrids as potential anti-ischemic agents
Wu, Jianbing,Yin, Wei,Zhang, Yinqiu,Ye, Hui,Li, Yunman,Tian, Jide,Huang, Zhangjian,Zhang, Yihua
, p. 1881 - 1886 (2020)
To improve aqueous solubility and anti-ischemic activity of 3-n-butylphthalide (NBP), we designed and synthesized the ring-opened derivative of NBP-ferulic acid-glucose trihybrids (S1-S8). These hybrids inhibited adenosine diphosphate (ADP)- or arachidonic acid (AA)-induced platelet aggregation, among them, S2 was 30-fold more water-soluble, and over 10-fold more potent in inhibition of platelet aggregation, as well as reduced ROS generation and protected primary neuronal cells from OGD/R-induced damage, in comparison with NBP. Additionally, S2 was more active than its three moieties alone or in combination, suggesting that the activity of S2 may be attributed to the synergistic effects of these moieties. Importantly, in vivo studies indicated that S2 not only possessed good pharmacokinetic profile, but also improved NBP distribution in rodent brain, suggesting that the glucose moiety in S2 may be recognized by glucose transporter 1 (GLUT1) on blood-brain barrier (BBB), promoting it to penetrate through BBB. Our findings suggest that S2 may be a promising candidate for the intervention of ischemic stroke, warranting further study.
Novel brain-targeting 3-n-butylphthalide prodrugs for ischemic stroke treatment
Xiang, Honglin,Zhang, Qiang,Han, Yikun,Yang, Lan,Zhang, Yan,Liu, Qiang,Zhang, Zhirong,Zhang, Ling
, p. 498 - 514 (2021)
Currently, ischemic stroke is the leading cause of disability and death worldwide, and the performance of corresponding drugs is often unsatisfactory owing to the complex pathological processes and the impediment of the blood-brain barrier (BBB). Here, we
Butylphthalide ring-opening derivative as well as preparation method and application thereof
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, (2021/09/21)
The invention relates to a butylphthalide ring-opening derivative and a preparation method and application thereof. The butylphthalide ring-opening derivative can significantly improve the ischemia symptom of the cerebral ischemia reperfusion model rat, a
Prodrug based on butylphthalide structure or pharmaceutically acceptable metal salt thereof as well as preparation method and application thereof
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Paragraph 0018; 0041-0042; 0044-0045, (2021/04/21)
The invention discloses a prodrug based on a butylphthalide structure or a pharmaceutically acceptable metal salt thereof, wherein the structural general formula I is shown in the specification; the prodrug can stably target a gastrointestinal monocarboxy
BUTYLPHTHALIDE-TELMISARTAN HETEROCOMPLEX, PREPARATION METHOD AND APPLICATION THEREOF
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, (2019/12/30)
The invention discloses a butylphthalide-telmisartan heterocomplex, a preparation method and an application thereof. The invention specifically relates to an optically active ring-opening butylphthalide-telmisartan heterocomplex shown in formula I or a ph
Ginkgolide B Derivative and Preparation Method And Use Thereof
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Paragraph 0046, (2019/03/30)
Disclosed are a compound as shown in formula I or formula II or a pharmaceutically acceptable salt thereof, wherein R1 is selected from pyrazinyl or substituted pyrazinyl; and R2 is selected from pyrazinyl or substituted pyrazinyl, phenyl or substituted phenyl, alkyl or substituted alkyl.
Salts prepared from 2-(1-acyloxy-n-amyl)benzoic acid and basic amino acid or aminoguanidine, and preparation method and application thereof
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Paragraph 0067; 0068, (2019/05/08)
The invention discloses salts prepared from 2-(1-acyloxy-n-amyl)benzoic acid and basic amino acid or aminoguanidine, a preparation method thereof, a medicinal preparation containing the salts, and application of the salts to preparing of medicines used fo
Organic amine ester derivative drug of 2-(alpha hydroxyl amyl) benzoic acid
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, (2018/11/22)
The invention discloses a preparation method and an application of an organic amine derivative drug of 2-(alpha hydroxyl amyl) benzoic acid, and particularly relates to a compound shown as general formula I as shown in the specification, or pharmaceutical
Novel hybrids of 3-n-butylphthalide and edaravone: Design, synthesis and evaluations as potential anti-ischemic stroke agents
Sheng, Xiao,Hua, Kai,Yang, Chunyu,Wang, Xiaoli,Ji, Hui,Xu, Jinyi,Huang, Zhangjian,Zhang, Yihua
, p. 3535 - 3540 (2015/08/06)
Abstract Fourteen hybrids (10a-g, 11a-g) of 3-n-butylphthalide (NBP) and edaravone (Eda) analogues have been designed and synthesized as potential anti-ischemic stroke agents. In vitro biological studies showed that compounds 10d and 10g exhibited more potent anti-platelet aggregation than ticlopidine (Ticlid), aspirin (ASP) and NBP. Compound 10g more significantly prevented H2O2-mediated neuronal cell (PC12) death than NBP, Eda or NBP together with Eda. Meanwhile, 10g also possessed potent radical scavenging effects on hydroxyl radical (·OH) and superoxide anion radical (·O2-). Our findings may provide new insights into the development of these hybrids, like 10g, for the intervention of ischemic stroke.
Design, synthesis and biological evaluation of hydrogen sulfide releasing derivatives of 3-n-butylphthalide as potential antiplatelet and antithrombotic agents
Wang, Xiaoli,Wang, Linna,Sheng, Xiao,Huang, Zhangjian,Li, Tingting,Zhang, Ming,Xu, Jinyi,Ji, Hui,Yin, Jian,Zhang, Yihua
, p. 5995 - 6004 (2014/08/05)
In the present study, a series of hydrogen sulfide (H2S) releasing derivatives (8a-g and 9a-f) of 3-n-butylphthalide (NBP) were designed, synthesized and biologically evaluated. The most promising compound 8e significantly inhibited the adenosi
