Taha Muhammad, Irshad Maryam, Imran Syahrul, Chigurupati Sridevi, Selvaraj Manikandan, Rahim Fazal, Ismail Nor Hadiani, Nawaz Faisal, Khan Khalid Mohammed
Department of Clinical Pharmacy, Institute for Research and Medical Consultations (IRMC), University of Dammam, Dammam 31441, Saudi Arabia.
Department of Chemistry, University of Wah, Quaid Avenue, Wah Cantt 47000, Pakistan; Atta-ur-Rahman Institute for Natural Product Discovery, Universiti Teknologi MARA (UiTM), Puncak Alam Campus, 42300 Bandar Puncak Alam, Selangor, Malaysia.
Eur J Med Chem. 2017 Dec 1;141:530-537. doi: 10.1016/j.ejmech.2017.10.028. Epub 2017 Oct 12.
Piperazine Sulfonamide analogs (1-19) have been synthesized, characterized by different spectroscopic techniques and evaluated for α-amylase Inhibition. Analogs 1-19 exhibited a varying degree of α-amylase inhibitory activity with IC values ranging in between 1.571 ± 0.05 to 3.98 ± 0.397 μM when compared with the standard acarbose (IC = 1.353 ± 0.232 μM). Compound 1, 2, 3 and 7 showed significant inhibitory effects with IC value 2.348 ± 0.444, 2.064 ± 0.04, 1.571 ± 0.05 and 2.118 ± 0.204 μM, respectively better than the rest of the series. Structure activity relationships were established. Molecular docking studies were performed to understand the binding interaction of the compounds.
已合成哌嗪磺酰胺类似物（1-19），通过不同光谱技术对其进行表征，并评估其对α-淀粉酶的抑制作用。与标准阿卡波糖（IC = 1.353±0.232 μM）相比，类似物1-19表现出不同程度的α-淀粉酶抑制活性，IC值在1.571±0.05至3.98±0.397 μM之间。化合物1、2、3和7显示出显著的抑制作用，IC值分别为2.348±0.444、2.064±0.04、1.571±0.05和2.118±0.204 μM，优于该系列中的其他化合物。建立了构效关系。进行了分子对接研究以了解化合物的结合相互作用。
