biostudies-literatureUnknown14(49)Sethi ASugar mimics are valuable tools in medicinal chemistry, offering the potential to overcome the limitations of carbohydrate inhibitors, such as poor pharmacokinetics and non-selectivity. In our continued efforts to develop heterocyclic galectin-1 inhibitors, we report the synthesis and characterization of thiazole-linked coumarin piperazine hybrids (10a-10i) as Gal-1 inhibitors. The compounds were characterized using ¹H NMR, ¹³C NMR and HRMS. Among the synthesized molecules, four compounds demonstrated significant inhibitory activity, with more than 50% inhibition observed at a concentration of 20 μM in a Gal-1 enzyme assay. Fluorescence spectroscopy was further utilized to elucidate the binding constant for the synthesized compounds. 10g exhibited the highest affinityRSC advances36794-36803https://www.ebi.ac.uk/biostudies/studies/S-EPMC11571122biostudies-literatureSugar mimics and their probable binding sites: design and synthesis of thiazole linked coumarin-piperazine hybrids as galectin-1 inhibitors.PMC11571122Sethi AKumar JAlvala MVemula DQureshi IAGadde DTalla VfalseSugar mimics and their probable binding sites: design and synthesis of thiazole linked coumarin-piperazine hybrids as galectin-1 inhibitors.Sugar mimics are valuable tools in medicinal chemistry, offering the potential to overcome the limitations of carbohydrate inhibitors, such as poor pharmacokinetics and non-selectivity. In our continued efforts to develop heterocyclic galectin-1 inhibitors, we report the synthesis and characterization of thiazole-linked coumarin piperazine hybrids (10a-10i) as Gal-1 inhibitors. The compounds were characterized using ¹H NMR, ¹³C NMR and HRMS. Among the synthesized molecules, four compounds demonstrated significant inhibitory activity, with more than 50% inhibition observed at a concentration of 20 μM in a Gal-1 enzyme assay. Fluorescence spectroscopy was further utilized to elucidate the binding constant for the synthesized compounds. 10g exhibited the highest affinity2024-01-01T00:00:00Z2024 Nov2026-06-02T04:02:38.487Z2025-04-21T21:41:12.969ZS-EPMC115711223955957610.1039/d4ra06715k