HEJ Research Institute of Chemistry, International Centre for Chemical & Biological Sciences, University of Karachi, Karachi, 75270, Pakistan.
Department of Clinical Pharmacy, Institute for Research & Medical Consultations (IRMC), Imam Abdulrahman Bin Faisal University, Dammam, 31441, Saudi Arabia.
Future Med Chem. 2023 Jan;15(2):167-187. doi: 10.4155/fmc-2022-0247. Epub 2023 Feb 17.
Identification of molecules having dual capabilities to reduce postprandial hyperglycemia and oxidative stress is one of the therapeutic approaches to treat diabetes mellitus. In this connection, a library of benzofuran-linked chalcone derivatives were evaluated for their dual action. A series of substituted benzofuran-linked chalcones () were synthesized and tested for α-amylase inhibitory as well as 2,2-diphenylpicrylhydrazyl (DPPH) and 2,2'-azino-(3-ethylbenzothiazoline-6-sulfonic acid) (ABTS) radical scavenging activities. All compounds showed α-amylase inhibitory activity ranging from IC = 12.81 ± 0.03 to 87.17 ± 0.15 μM, compared with the standard acarbose (IC = 13.98 ± 0.03 μM). Compounds also demonstrated radical scavenging potential against DPPH and ABTS radicals. The identified compounds may serve as potential leads for further advanced research.
鉴定具有降低餐后高血糖和氧化应激双重作用的分子是治疗糖尿病的一种治疗方法。在这方面，评估了苯并呋喃连接的查尔酮衍生物库的双重作用。合成了一系列取代的苯并呋喃连接的查尔酮（），并测试了它们对α-淀粉酶的抑制作用以及 2,2-二苯基-1-苦肼基（DPPH）和 2,2'-联氮基-（3-乙基苯并噻唑啉-6-磺酸）（ABTS）自由基清除活性。与标准阿卡波糖（IC = 13.98 ± 0.03 μM）相比，所有化合物均显示出对α-淀粉酶的抑制活性，范围为 IC = 12.81 ± 0.03 至 87.17 ± 0.15 μM。化合物还表现出对 DPPH 和 ABTS 自由基的清除潜力。鉴定出的化合物可能作为进一步深入研究的潜在先导化合物。
