Studies on the total synthesis of metabolites of nootropics KMBZ-009 and their bioactivity

  The project was supported by NSFC.

  Abstract:Studies on metaboltes of KMBZ-009 had been carried in the accordance with the  results of animal pharmacokinetics,in recent research and development of nootropic KMBZ-009. In our work, metabolites M1, M2, M3 and M4 were designed and synthesized, and their activity of calcium antagonism were the same or lower than that of KMBZ-009 with respect to inhibition of either potential-dependance calcium channel or receptor-dependance calcium channels. From this piont, it is presumed that bioactivity of KMBZ-009 related to calcium antagonism in vivo  was resulted by itself. As the result of this work, the importent evidences were provided for studies on  clinic trial of KMBZ-009 and discussion with its structure-activity relationship, and also development of other candidates for new drug.


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