STRUCTURAL MODIFICATION AND BIOACTIVITY OF PERLOLYRINE

AIM: To search for compounds for the treatment of cardiovascular diseases. METHODS: According to rational drug design principle, a series of analogues of perlolyrine were prepared, and the antiplatelet aggregation activity and antithrombotic effects of these compounds were tested. RESULTS: Sixteen perlolyrine analogues were synthsized(I～XVI). Of them, 8 compounds(I,II,V～VII,IX,XI and XV) were first reported. CONCLUSION: All synthesized compounds showed antiplatelet aggregation activity to a certain degree. Of them, 8 compounds(I～IV,VII,X,XI and XIII) exhibited antithrombotic effects.