Development of Malarial Enzyme Inhibitors
Elīna Līdumniece, Riga Technical University, Latvia
The research presented in the Thesis describes the development of synthesis methods to obtain peptidic boronic acid SUB1 inhibitors. The established synthetic routes enabled an access of various peptidic boronic acids with modified P1, P3 and P5 positions. The newly synthesized inhibitors were evaluated for their ability to inhibit SUB1 as well as for their antimalarial potency in cell-based assays and in vitro selectivity counter screen tests. The research has resulted in a series of compounds with low nanomolar inhibitory potency in SUB1 enzymatic assays, several of which displayed sub-micromolar inhibitory potency in P. falciparum parasite growth tests.
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