1085474-04-9Relevant 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)
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.
Salts prepared from 2-(1-acyloxy-n-amyl)benzoic acid and basic amino acid or aminoguanidine, and preparation method and application thereof
-
Paragraph 0085; 0086; 0090-0092, (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
