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Synthesis of scutellarin derivatives and study of their anti-heart ischemia activities in rats
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DOI   10.11656/j.issn.1672-1519.2010.03.32
Key Words   scutellarin;synthesis;heart ischemia;structure-activity relationship
Author NameAffiliation
YANG Li-mei Pharmaceutial college, Tianjin Medical University, Tianjin 300070, China 
GU Jun Department of Pharmaceutical Chemistry, Medical Collage of Chinese People’s armed Police, Tianjin 300162, China
Tianjin Key Laboratory of Occupational and Environmental Hazards 
LI Jian-yu Department of Pharmaceutical Chemistry, Medical Collage of Chinese People’s armed Police, Tianjin 300162, China
Tianjin Key Laboratory of Occupational and Environmental Hazards 
代皓 Department of Pharmaceutical Chemistry, Medical Collage of Chinese People’s armed Police, Tianjin 300162, China 
李灵芝 Department of Pharmaceutical Chemistry, Medical Collage of Chinese People’s armed Police, Tianjin 300162, China
Tianjin Key Laboratory of Occupational and Environmental Hazards 
Abstract
    [Objection] To design and synthesize a series of scutellarin derivatives for searching for their structure-activity relationship of protective effects on heart ischemia in Rats.[Methods] Using scutellarin as staring material,a series of ether derivatives based on scutellarein gained from scutellarin’s hydrolysis were synthesized by reacting with kinds of alkylogen,and then these compounds were evaluated for protective effects on Ischemic myocardial cells in Rats using MTT assay in vitro.[Results]The 3 intermediates and 13 target compounds were synthesized.The protection effect of compound 2,4,5 to ischemic myocardial cells in rats was better than the positive control.[Conclusion] The glucuronyl in the structure had little dedication on the activities of scutellarin while the 4’-OH was essential.

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