In search of novel antiplatelet agents, the naturally-occurring gingerdiones (20, 24) were selected as lead compounds. A series of their derivatives were synthesized and screened for antiplatelet activity. It was found that all of the synthesized gingerdione derivatives demonstrated potent inhibition against AA-induced platelet aggregation. Among them, -gingerdione (18) and -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-1 and COX-2 inhibition. The exact mechanism of action of these new compounds should be further investigated.
|Number of pages||11|
|Journal||Chinese Pharmaceutical Journal|
|Publication status||Published - 2002 Aug 1|
All Science Journal Classification (ASJC) codes
- Pharmaceutical Science