发明名称 |
TRYPTAMINE DERIVATIVES, THEIR PREPARATION AND THEIR USE IN GASTROPATHY |
摘要 |
The synthesis and evaluation of gastroprotective effect of different tryptamine derivatives. Tryptamine derivatives have been synthesized 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 synthesized 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 also 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 mitochondroial transmembrane potential and dehydrogenase activity. SEGA (3a) plays an important role as an iron chelator as well as intra mitochondrial ROS scavenger. Thus, SEGA (3a) is a potent antioxidant antiapototic molecule, which efficiently prevents NSAID-induced gastropathy and stress or alcohol-mediated gastric damage.
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申请公布号 |
US2013197052(A1) |
申请公布日期 |
2013.08.01 |
申请号 |
US201113822463 |
申请日期 |
2011.09.14 |
申请人 |
BANDYOPADHYAY UDAY;PAL CHINMAY;BINDU SAMIK;ADHIKARI SUSANTA SEKHAR;UNIVERSITY OF CALCUTTA;COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCH |
发明人 |
BANDYOPADHYAY UDAY;PAL CHINMAY;BINDU SAMIK;ADHIKARI SUSANTA SEKHAR |
分类号 |
C07D209/16 |
主分类号 |
C07D209/16 |
代理机构 |
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代理人 |
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