Abstract
In this study synthesis and β-glucuronidase inhibitory potential of 3/5/8 sulfonamide and 8-sulfonate derivatives of quinoline (1–40) are discussed. Studies reveal that all the synthetic compounds were found to have good inhibitory activity against β-glucuronidase. Nonetheless, compounds 1, 2, 5, 13, and 22–24 having IC50 values in the range of 1.60–8.40 μM showed superior activity than the standard saccharic acid 1,4-lactone (IC50 = 48.4 ± 1.25 μM). Moreover, molecular docking studies of selected compounds were also performed to see interactions between active compounds and binding sites. Structures of all the synthetic compounds were confirmed through 1H NMR, EI-MS and HREI-MS spectroscopic techniques.
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•Syntheses of sulfonamide and sulfonate derivatives of quinolines have been carried out.•All synthetic compounds were characterized by spectroscopic techniques.•β-Glucuronidase inhibitory of synthetic compounds has been carried out.•Docking studies of active analogs have been performed.•Structure-activity relationship has been evaluated.