Y. Lai, L. J. Huang, Hsien‐Cheng Lin, Tian-Shung Wu, C. Teng, S. Kuo
{"title":"Synthesis of Gingerdione Derivatives as Potent Antiplatelet Agents","authors":"Y. Lai, L. J. Huang, Hsien‐Cheng Lin, Tian-Shung Wu, C. Teng, S. Kuo","doi":"10.7019/CPJ.200208.0259","DOIUrl":null,"url":null,"abstract":"In search of novel antiplatelet agents, the naturally-occurring gingerdiones (20, 24) were selected as lead com pounds. A series of their derivatives were synthesized and screened for anti-platelet activity. It was found that all of the synthesized gingerdione derivatives demonstrated potent inhibition against AA-induced platelet aggregation. Among them, 141-gingerdione (I8) and 51-gingerdione (19) showed the highest potency, being about 1/3 and one time as potent as indomethacin, respectively. Preliminary studies indicated that the mechanism of action of these gingerdione derivatives differed from indomethacin. Unlike indomethacin, they showed no appreciable COX-I and COX-2 inhibition. The exact mechanism of action of these new compounds","PeriodicalId":22409,"journal":{"name":"The Chinese Pharmaceutical Journal","volume":"55 1","pages":"259-269"},"PeriodicalIF":0.0000,"publicationDate":"2002-08-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"3","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"The Chinese Pharmaceutical Journal","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.7019/CPJ.200208.0259","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
引用次数: 3
Abstract
In search of novel antiplatelet agents, the naturally-occurring gingerdiones (20, 24) were selected as lead com pounds. A series of their derivatives were synthesized and screened for anti-platelet activity. It was found that all of the synthesized gingerdione derivatives demonstrated potent inhibition against AA-induced platelet aggregation. Among them, 141-gingerdione (I8) and 51-gingerdione (19) showed the highest potency, being about 1/3 and one time as potent as indomethacin, respectively. Preliminary studies indicated that the mechanism of action of these gingerdione derivatives differed from indomethacin. Unlike indomethacin, they showed no appreciable COX-I and COX-2 inhibition. The exact mechanism of action of these new compounds