Kasturi Sivaprasad, Surarapu Sujatha, Bathoju Chandra Chary, Uppalanchi Srinivas, Dwivedi Shubham, Perumal Yogeeswari, Sigalapalli Dilep Kumar, Babu Bathini Nagendra, Ethiraj Krishna S, Anireddy Jaya Shree
Department of Medicinal Chemistry , GVK Biosciences Pvt. Ltd , Plot.No.28 A, IDA, Nacharam , Hyderabad 500076 , Telangana State , India.
Centre for Chemical Sciences & Technology , Institute of Science and Technology , JNTUH, Kukatpally , Hyderabad 500085 , Telangana State , India . Email:
Medchemcomm. 2017 Jun 14;8(8):1618-1630. doi: 10.1039/c7md00162b. eCollection 2017 Aug 1.
An efficient acid catalyzed methodology has been employed to synthesize a variety of aza-flavanones and their α-glucosidase inhibitory activity is evaluated using acarbose, miglitol and voglibose as reference standards. Molecular modeling studies were performed for all compounds to identify the important binding modes responsible for the inhibition activity of α-glucosidase which helped find key interactions between the enzyme and the active compounds. Among all the compounds , and have shown high α-glucosidase inhibition activity compared to standard reference drugs and have been identified as promising potential antidiabetic agents. This study is the first biological evaluation of aza-flavanones as α-glucosidase inhibitors.
一种高效的酸催化方法已被用于合成多种氮杂黄酮，并且以阿卡波糖、米格列醇和伏格列波糖作为参考标准评估了它们的α-葡萄糖苷酶抑制活性。对所有化合物进行了分子模拟研究，以确定导致α-葡萄糖苷酶抑制活性的重要结合模式，这有助于发现酶与活性化合物之间的关键相互作用。在所有化合物中，[此处原文缺失具体化合物信息]与标准参考药物相比显示出较高的α-葡萄糖苷酶抑制活性，并已被确定为有前景的潜在抗糖尿病药物。这项研究是对氮杂黄酮作为α-葡萄糖苷酶抑制剂的首次生物学评估。
