| abstract |
The invention relates to tetrahydrothienopyridine deuterated derivatives, a preparation method and medicinal application thereof, and belongs to the field of medicinal chemistry. Said derivatives include salts of compounds of formula I and enantiomers and racemates of compounds of formula I. The results of in vitro whole blood hydrolysis experiments show that the compound of formula I has better stability to esterase, and the hydrolysis rate of its carboxylate methyl ester is significantly slower than that of non-deuterated methyl ester. The compound of formula I of the present invention can be effectively converted into a pharmacologically active metabolite in vivo to exert its effect of inhibiting platelet aggregation, and the concentration of the active metabolite is significantly higher than that of clopidogrel or a non-deuterated compound of corresponding structure. The results of pharmacodynamic experiments show that the compound of formula I of the present invention has significant platelet aggregation inhibitory effect, and the anti-platelet aggregation effect is obviously better than clopidogrel and non-deuterated compounds with corresponding structures. Therefore, the compound of formula I of the present invention can be used to prepare medicines for preventing or treating thrombosis and embolism-related diseases. |