Synthesis and biological activity of aspirin derivatives.
Aspirin has been widely used as analgesic and anti-inflammatory drug. Recently, it was elucidated that aspirin have anti-coaggregatory effect in low dose. This study was carried out to investigate the synthesis of aspirin derivatives from aspirin and aromatic compound of antioxidant and its biological activities. Synthesis of aspirin derivatives was prepared by esterification in the presence of 1,1-carbonyldiimidazole. Biological activities was examined using effect of anti-coagulant on bleeding time, effect of antioxidant and effect of anti-platelet aggregation. As a result, SJ-101 showed strong antioxidative activity and anti-coagulant activity among four compounds. Anti-platelet aggregation of SJ-101 was examined by collagen, ADP, PAF method. SJ-101 exhibited more stronger activity to aspirin at collagen aggregation reaction. These finding demonstrates that SJ-101 is useful as care drug of aging and old-disease because of its has antioxidant activity, anti-coagulant activity and anti-platelet activity.
Cha
B C
BC
Department of Applied Animal Sciences, College of Life Sciences and Natural Resources, Sangji University, Wonju, Korea. bccha@chiak.sangji.ac.kr
Lee
S B
SB
D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis* / Q000494:pharmacology*; D000975:Antioxidants / Q000138:chemical synthesis / Q000494:pharmacology; D001241:Aspirin / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000494:pharmacology*; D001760:Bleeding Time; D066298:In Vitro Techniques; D007202:Indicators and Reagents; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D010636:Phenols / Q000138:chemical synthesis / Q000494:pharmacology; D010974:Platelet Aggregation / Q000187:drug effects; D011817:Rabbits; D051381:Rats; D013056:Spectrophotometry, Ultraviolet
D000894:Anti-Inflammatory Agents, Non-Steroidal; D000975:Antioxidants; D007202:Indicators and Reagents; D010636:Phenols; D001241:Aspirin