Abstract
We have previously shown that azasterols have activity against Trypanosoma brucei, Trypanosoma cruzi and Leishmania species, which are the causative agents of various neglected tropical diseases. In this paper, we discuss the replacement of the sterol core of the azasterols with sterol mimics. Various mimics were designed, and the structures were minimised to see if they could adopt a similar conformation to that of the azasterols. From this, two series of mimics were synthesised and then evaluated against the parasites. Compounds showed moderate activity. (C) 2010 Elsevier Ltd. All rights reserved.
| Original language | English |
|---|---|
| Pages (from-to) | 7291-7301 |
| Number of pages | 11 |
| Journal | Bioorganic & Medicinal Chemistry |
| Volume | 18 |
| Issue number | 20 |
| DOIs | |
| Publication status | Published - 15 Oct 2010 |
UN SDGs
This output contributes to the following UN Sustainable Development Goals (SDGs)
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SDG 3 Good Health and Well-being
Keywords
- Trypanosoma
- Leishmania
- Azasterol
- HIGH-ENERGY INTERMEDIATE
- ESTROGEN-RECEPTOR
- TRYPANOSOMA-BRUCEI
- AZASTEROLS
- INHIBITION
- ANALOGS
- METHYLTRANSFERASE
- BIOSYNTHESIS
- DERIVATIVES
- BINDING
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