Abstract

The anti-inflammatory properties of β-carbolines have been widely studied, highlighting their potential in treating inflammatory disorders. This research investigates the anti-inflammatory activity of selected 1-substituted glyoxal β-carboline derivatives, achieved through a one-step conversion of 5-hydroxy-L-tryptophan with activated glyoxal, without forming tetrahydro-β-carboline (THβC) intermediates. These derivatives (4e-g) were synthesized successfully without requiring expensive metal catalysts, prolonged reaction times, or stringent reaction conditions, and yielded moderate amounts. Our findings indicate that all the derivatives significantly inhibit xanthine oxidase (XO) activity, leading to a reduction in reactive oxygen species (ROS) and free radicals. This inhibition disrupts the inflammatory cascade and attenuates the inflammatory response.

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