HEJ Research Institute of Chemistry, International Center for Chemical & Biological Sciences, University of Karachi, Karachi, 75270, Pakistan.
Department of Chemistry, University of Malakand, Chakdara Dir, Khyber Pakhtunkhwa, 18800, Pakistan.
Future Med Chem. 2023 Mar;15(6):497-515. doi: 10.4155/fmc-2022-0317. Epub 2023 Apr 24.
In medicinal chemistry, searching for new therapeutic entities to treat diabetes mellitus is of great concern. The piperidinyl-substituted chalcone scaffold has piqued our interest as a potential antidiabetic agent. A variety of piperidinyl-substituted chalcones were synthesized and tested for α-amylase inhibitory and 2,2-diphenyl-1-picrylhydrazyl and 2,2'-azino-(3-ethylbenzothiazoline-6-sulfonic acid) radical-scavenging activities. Compared with the standard acarbose, all compounds inhibited α-amylase, with IC values of 9.86-35.98 μM. Docking studies revealed an important binding interaction with the enzyme's catalytic site. The compounds also demonstrated promising radical-scavenging potential against 2,2-diphenyl-1-picrylhydrazyl and 2,2'-azino-(3-ethylbenzothiazoline-6-sulfonic acid) radicals. This study has identified potential lead candidates for further advanced research searching for antidiabetic agents.
在药物化学中，寻找新的治疗糖尿病的治疗实体是非常关注的。哌啶基取代的查耳酮骨架作为一种潜在的抗糖尿病药物引起了我们的兴趣。合成了多种哌啶基取代的查尔酮，并对其α-淀粉酶抑制作用和 2,2-二苯基-1-苦基肼基（DPPH）自由基清除活性进行了测试。与标准阿卡波糖相比，所有化合物均抑制α-淀粉酶，IC 值为 9.86-35.98 μM。对接研究表明，化合物与酶的催化部位存在重要的结合相互作用。这些化合物对 2,2-二苯基-1-苦基肼基（DPPH）和 2,2'-偶氮-(3-乙基苯并噻唑啉-6-磺酸)自由基也表现出有希望的清除活性。这项研究为进一步寻找抗糖尿病药物的研究确定了潜在的先导候选物。
