380905-53-3Relevant academic research and scientific papers
Novel hybrids of optically active ring-opened 3-n-butylphthalide derivative and isosorbide as potential anti-ischemic stroke agents
Wang, Xiaoli,Wang, Linna,Li, Tingting,Huang, Zhangjian,Lai, Yisheng,Ji, Hui,Wan, Xiaolong,Xu, Jinyi,Tian, Jide,Zhang, Yihua
, p. 3078 - 3089 (2013/05/23)
In search of novel anti-ischemic stroke agents with higher potency than a known drug 3-n-butylphthalide (NBP), a series of hybrids ((S)- and (R)-5a-f) from optically active ring-opened NBP derivative and isosorbide were synthesized for evaluating their anti-ischemic stroke activity. Compound (S)-5e displayed the strongest activity in inhibiting the adenosine diphosphate (ADP) and arachidonic acid (AA)-induced platelet aggregation in vitro, with 10.0- and 8.4-fold more effectiveness than (S)-NBP, respectively. Furthermore, (S)-5e was stable in artificial gastrointestinal fluids and could penetrate the blood-brain barrier (BBB) with an appreciate lipid/water partition coefficient relative to (S)-NBP. More importantly, oral treatment with (S)-5e protected from acute thrombosis and inhibited the ischemia/reperfusion-related brain injury in animals. Our findings suggest that (S)-5e may be promising for further evaluation for the intervention of ischemic stroke.
Studies on the enantiomers of ZJM-289: Synthesis and biological evaluation of antiplatelet, antithrombotic and neuroprotective activities
Wang, Xiaoli,Zhao, Qian,Wang, Xuliang,Li, Tingting,Lai, Yisheng,Peng, Sixun,Ji, Hui,Xu, Jinyi,Zhang, Yihua
, p. 9030 - 9040 (2013/01/15)
ZJM-289 is a potent racemic agent which inhibits both platelet aggregation and thrombosis superior to a known anti-ischemic stroke drug 3-n-butylphthalide (NBP). Herein, the enantiomers of ZJM-289, (S)-ZJM-289 and (R)-ZJM-289, were synthesized and evaluat
Synthesis, resolution, and antiplatelet activity of 3-substituted 1(3H)-isobenzofuranone
Yang, Hua,Hu, Gao-Yun,Chen, Jun,Wang, Yi,Wang, Zhong-Hua
, p. 5210 - 5213 (2008/02/11)
A series of 3-substituted-1(3H)-isobenzofuranone 6a-g and 7a-g were synthesized from phthalic anhydride. The compound 6a-g was resolved. The antiplatelet activities of these compounds were evaluated using in vitro experiment of platelet aggregation. The levels of antiplatelet activity were displayed as following sequence: l-isomer > dl-isomer > d-isomer, respectively. The alkylphthalide is more active than the corresponding alkenephthalide. All these compounds were less active than n-butylphthalide (NBP, 6c) and Aspirin (Asp).
