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  • Title: Pharmacomodulation on the 3-acetylursolic acid skeleton: Design, synthesis, and biological evaluation of novel N-{3-[4-(3-aminopropyl)piperazinyl]propyl}-3-O-acetylursolamide derivatives as antimalarial agents.
    Author: Gnoatto SC, Susplugas S, Dalla Vechia L, Ferreira TB, Dassonville-Klimpt A, Zimmer KR, Demailly C, Da Nascimento S, Guillon J, Grellier P, Verli H, Gosmann G, Sonnet P.
    Journal: Bioorg Med Chem; 2008 Jan 15; 16(2):771-82. PubMed ID: 17967541.
    Abstract:
    A series of new piperazine derivatives of ursolic acid was synthesized and tested against Plasmodium falciparum strains. They were also tested on their cytotoxicity effects upon MRC-5 cells. Seven new piperazinyl analogues showed significant activity in the nanomolar range (IC(50)=78-167nM) against Plasmodium falciparum CQ-resistant strain FcB1. A possible mechanism of interaction implicating binding of these compounds to beta-hematin was supported by in vitro tests. Moreover, the importance of the hydrophilic framework attached at the terminal nitrogen atom of the bis-(3-aminopropyl)piperazine joined to the triterpene ring was also explored through molecular dynamic simulations.
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