Khan Khalid Mohammed, Rahim Fazal, Wadood Abdul, Kosar Naveen, Taha Muhammad, Lalani Salima, Khan Aisha, Fakhri Muhammad Imran, Junaid Muhammad, Rehman Wajid, Khan Momin, Perveen Shahnaz, Sajid Muhammad, Choudhary M Iqbal
H.E.J. Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi 75270, Pakistan.
Department of Chemistry, Hazara University, Mansehra, Pakistan.
Eur J Med Chem. 2014 Jun 23;81:245-52. doi: 10.1016/j.ejmech.2014.05.010. Epub 2014 May 4.
In our effort directed toward the discovery of new anti-diabetic agent for the treatment of diabetes, a library of biscoumarin derivative 1-18 was synthesized and evaluated for α-glucosidase inhibitory potential. All eighteen (18) compounds displayed assorted α-glucosidase activity with IC50 values 16.5-385.9 μM, if compared with the standard acarbose (IC50 = 906 ± 6.387 μM). In addition, molecular docking studies were carried out to explore the binding interactions of biscoumarin derivatives with the enzyme. This study has identified a new class of potent α-glucosidase inhibitors.
在我们致力于发现用于治疗糖尿病的新型抗糖尿病药物的过程中，合成了双香豆素衍生物1 - 18库，并对其α - 葡萄糖苷酶抑制潜力进行了评估。与标准阿卡波糖（IC50 = 906 ± 6.387 μM）相比，所有十八种（18）化合物均表现出不同的α - 葡萄糖苷酶活性，IC50值为16.5 - 385.9 μM。此外，还进行了分子对接研究，以探索双香豆素衍生物与该酶的结合相互作用。这项研究确定了一类新的强效α - 葡萄糖苷酶抑制剂。
