US8901317: Tryptamine derivatives, their preparation and their use in gastropathy

The invention concerns the synthesis and evaluation of gastroprotective effect of different tryptamine derivatives. Tryptamine derivatives have been synthesised by formation of amide or ester with some known anti-oxidant molecules. These derivatives show excellent antioxidant property in-vitro among all the derivatives, the compound SEGA (3a), that was prepared by the combination of serotonin with gallic acid shows the greater antioxidant property than the other synthesised compounds both in vivo and in vitro. SEGA(3a) shows the gastroprotective effect against NSAIDs (indomethacin or diclofenac)-induced gastropathy in dose dependent manner and accelerates the healing from injury. It prevents the NSAIDs-induced mitochondrial oxidative stress in vivo. This derivative prevents NSAID-induced mitochondrial oxidative stress-mediated apoptosis in vivo by preventing the activation of caspase 9 and caspase-3 and restores NSAIDs-mediated collapse of mitochondrial transmembrane potential and dehydrogenase activity. SEGA (3a) plays an important role as an iron chelator and intra mitochondrial ROS scavenger. Thus, SEGA (3a) is a potent antioxidant antiapoptotic molecule which efficiently prevents NSAID-induced gastropathy and stress or alcohol-mediated gastric damage.