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Synthesis Of Fused Heterocyclic Diamidines For The Treatment Of Human African Trypanosomiasis And Fluorescence Studies Of Selected Diamidines, Jennifer Crystal Brown Barber
Synthesis Of Fused Heterocyclic Diamidines For The Treatment Of Human African Trypanosomiasis And Fluorescence Studies Of Selected Diamidines, Jennifer Crystal Brown Barber
Chemistry Dissertations
A class of linear diamidines was synthesized for the evaluation as a treatment of Human African Trypanosomiasis. These fused heterocyclic compounds are thiazole[5,4-d]thiazoles and are of interest because the parent compound, 2,5-Bis(4-amidinophenyl)-thiazolo[5,4-d]thiazole HCl salt, which is also called DB 1929, has exhibited a low nanomolar IC50 value against Trypanosoma brucei rhodesiense and has shown selectivity for binding to the human telomere G-quadruplex over that of DNA duplex. A fluoro and a methoxy derivative have been synthesized and are currently undergoing testing for activity and binding affinity. In addition, fluorescence studies of selected diamidines were done to study the effect of …