Synthesis of Chalcones as Potential α-Glucosidase Inhibitors, In-Vitro and In-Silico Studies

Asma Mukhtar, Shazia Shah, Kanwal ,, Khalid Mohammed Khan*, Shahid Ullah Khan, Sumera Zaib, Jamshed Iqbal, Shahnaz Parveen, Muhammad Taha, Shafqat Hussain, Shahryar Hameed, Naveed Ahmed Khan*, Ruqaiyyah Siddiqui, Ayaz Anwar

*Corresponding author for this work

Research output: Contribution to journalArticlepeer-review

2 Citations (Scopus)


α-glucosidase inhibitors are potential antihyperglycemic agents. Seventeen chalcones derivatives (1–17) were synthesized by reactions of diversely substituted aldehydes with various ketones. The structures of compounds were characterized by using nuclear magnetic resonance (NMR) spectroscopy, mass spectrometry (MS) and carbon, hydrogen, nitrogen (CHN) analysis. These synthetic molecules were tested for α-glucosidase inhibitory activity. Acarbose was used as a standard drug and positive control in this study which exhibited an IC50 of 2.91±0.02 μM. Of seventeen, nine molecules 1-3, 5, 6, 8, and 11-13 displayed significant inhibition with IC50 values 1.19±0.19 to 15.79±0.99 μM. Compound 6 {(E)-3-(3,5-dichloro-2-hydroxyphenyl)-1-(p-tolyl)prop-2-en-1-one} with hydroxy and chloro substitutions was found to be the most active compound and a novel compound of this library with IC50=1.19±0.19 μM. Active molecules were subjected to in silico study to determine binding interactions with target site of α-glucosidase.
Original languageEnglish
Pages (from-to)9933-9940
Number of pages8
Issue number7
Early online date1 Oct 2021
Publication statusPublished - 6 Oct 2021


  • Dianetes
  • Enzyme models
  • Hyperglycemia
  • Structure-activity relationships


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