摘要
目的设计合成两个系列齐墩果酸衍生物,并对其进行体外降血糖活性评价。方法以齐墩果酸为先导物,经酰化、取代等反应得到目标化合物,并对目标化合物和阿卡波糖对α-葡萄糖苷酶的抑制活性进行对比。结果与结论合成了11个未见文献报道的新化合物,两个系列化合物的结构均经MS、1H-NMR谱确证。活性测定表明,目标化合物均具有一定的α-葡萄糖苷酶抑制活性,大部分齐墩果酸衍生物的活性高于齐墩果酸(IC50=0.502 mmol·L-1),其中,化合物6d对α-葡萄糖苷酶的抑制活性最高(IC50=0.025 mmol·L-1),为齐墩果酸的21倍。
Oleanic acid has a good hypoglycemic activity, but its bioavailability is low because of its poor solubility. So to find oleanic acid derivatives with better hypoglycemic activity and bioavailability became an important purpose in this study. Therefore two new series of oleanic acid derivatives coupled with amino acids and aminobenzoic acid were designed and synthesized from oleanic acid via acylation and substitution reaction, and their in vitro hypoglycemic effect were tested via evaluating the inhibitory activity against α- glucosidase. Eleven new compounds were obtained and their structures were characterized by MS and H-NMR spectra. Compared with the inhibition of oleanic acid （ IC5o = 0. 502 mmol. L-1 ） and arcarbose （IC50 = 0. 211 mmol. L- 1 ） against α-glucosidase, all compounds showed inhibitory activity, among which compound 6d performed the highest activity with the IC50 of 0. 025 mmol. L - 1
出处
《中国药物化学杂志》
CAS
CSCD
2014年第1期7-13,共7页
Chinese Journal of Medicinal Chemistry
基金
江苏省抗糖尿病药物筛选技术服务中心项目(BM2011117)
