SAR studies on azasterols as potential anti-trypanosomal and anti-leishmanial agents

Federica Gigante, Marcel Kaiser, Reto Brun, Ian H. Gilbert

    Research output: Contribution to journalArticlepeer-review

    20 Citations (Scopus)

    Abstract

    There is an urgent need for the development of new drugs for the treatment of neglected tropical diseases such as human African trypanosomiasis, Chagas disease and leishmaniasis. Azasterols, have been shown to have activity against the parasites which cause these diseases. In this paper we report synthesis of new azasterols and subsequent analysis of the SAR. The chemistry focused on variations in the ester at the 3 beta-position of the sterol and the position of the nitrogen in the side chain. The data allowed us to derive preliminary pharmacophore models for the activity of the azasterols against the parasites which cause these diseases. (C) 2009 Elsevier Ltd. All rights reserved.

    Original languageEnglish
    Pages (from-to)5950-5961
    Number of pages12
    JournalBioorganic & Medicinal Chemistry
    Volume17
    Issue number16
    DOIs
    Publication statusPublished - 15 Aug 2009

    Keywords

    • Trypanosomiasis
    • Leishmaniasis
    • Azasterols
    • DELTA-24-STEROL METHYLTRANSFERASE
    • TRYPANOSOMA-BRUCEI
    • CANDIDA-ALBICANS
    • SQUALAMINE
    • DERIVATIVES
    • INHIBITION
    • ANALOGS

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