Synthesis of tryptaminamides for In Vitro anti-inflammatory activity and subsequent In Silico analysis

Inflammation is a physiological response to tissue injury, characterized by redness, heat, swelling, and pain. Chronic, uncontrolled inflammation is associated with the development of diseases, such as Alzheimer’s disease, arthritis, asthma, atherosclerosis, Crohn’s disease, colitis, dermatitis, hepatitis, nephritis, etc. Conventional anti-inflammatory drugs are effective but often cause serious adverse effects, including gastrointestinal bleeding, ulceration, and perforation. In this study, a series of tryptaminamides was synthesized using derivatives of benzoic acid, including 2-chloro-5-nitrobenzoic acid, 4-nitrobenzoic acid, 2-chloro-4-nitrobenzoic acid, and 3-nitro-4-chlorobenzoic acid. Among the synthesized compounds, derivatives SJ0812, SJ0815, and SJ0817, containing both chloro and nitro-substituents, exhibited the highest in vitro anti-inflammatory activity, comparable to that of diclofenac. Subsequent in silico docking studies revealed additional binding pockets in the cyclooxygenase enzyme, suggesting opportunities for further structural optimization. These findings highlight the potential of tryptaminamide derivatives as a promising anti-inflammatory scaffold.