Synthesis Of Epigoitrin From L-ascorbic Acid And The Design, Synthesis, And Biological Evaluation Of Hybrids Of Praziquantel And Peroxide Containing Moieties As Anti-schistosomal Agents

This thesis includes two sections.First section:Synthesis of epigoitrin from L-Ascorbic Acid.Epigoitrin is the main bioactive constituent of an important traditional Chinese herbal medicineRadix Isatidis.Its antiviral, anticancer and antithyroid activities of epigoitrin had been reported.Extensive biological exploration of epigoitrin was constrained by the limited natural source. Fewmethods for the total synthesis of Epigoitrin were reported. Moreover, the reported methods are notpractical. This section describes our effort toward chemical preparation of epigoitrin from the readilyavailable L-Ascorbic acid. The target compound was characterized by1H NMR,13C NMR andHRMS.Second section: The design, synthesis, and biological evaluation of hybrids of praziquantel andperoxide containing moieties as anti-schistosomal agents.Schistosomiasis is an infectious disease that has been recognized as a severe health burden forsome regions of the world. While praziquantel is the drug of choice, there is a urgent need for thediscovery and development of novel antischistosomal compounds with higher efficacy and newmachnisms of action. DW-3-15had been reported as a novel and promising prodrug with goodefficacy agaist both adult and juvenile schistosomes. Here we report the synthesis and evaluation of aseries of DW-3-15based peroxide and praziquentel hybrid compounds. The antischistosomal activityof these compounds were evaluated both in vitro and in vivo.