Synthesis Of Levosimendan And Its Analogs And Research Of Their Activities In Anti-CHF

Pimobendan is a new inotropic agent with phosphodiesterase inhibiting and calcium-sensitizing effects . It came to the market in Japan in 1994. The present study indicated it can descend the pressure of vas effectually, increase left ventricular ejection fraction.Pimobendan has been as a racemic medicament from its appearance. For enantiomorphous often has different even contrary bio-activity, the study tried to synthesis levopimobendan based on the key levo intermediate's synthesis, and verify its better activity than its enantiomorphous's. Some derivatives of levopimobendan were synthesized and their activities were identified . The bio-activity of the target compounds were tested in blood pressure experiment. Results showed that the target compounds were effective to CHF by dilating blood vessel.For improving the reported synthetic route, levosimendan was synthesized from acetanilide via ten steps of reaction. Then with levopimobendan as a leading compound, 3 unreported compounds weredesigned and synthesized by structure modification of levosimendan, all with optic activity. The structures of the target compounds were identified by elemental analysis, MS, IR and 1H-NMR.The bio-activity of the target compounds were tested in blood pressure experiment, with levosimendan as a contrasting group. Results showed that the target compounds were effective to CHF by dilating blood vessel.