The Synthesis Of Danshensu Derivatives And Research Of Anti-hypoxia Activity

With tedious techenique, difficult extraction procedure and poor stability, danshensu, the half life of which is only 15min in injection, has no clinic value. According to pro-drug principl, the writer of this paper modified several sites of danshensu that are p-double hydroxyl, side chain a - hydroxyl and carboxilic, etc, which possibly effect the activity and stability of the mother structure, with reduce pressure hypoxia model of rat, the anti hypoxia activity of the derivatives prepared were tested after oral administration, to screen compounds which are high activity and stability after oral administration.12 compounds, belonging to three series, were synthesized in this paper, 11 of them are new compounds, whose structure were identified with 1H-NMR and MS. The pharmacological result showed 9 compounds have anti-hypoxia activity of different degree.