SAR studies on azasterols as potential anti-trypanosomal and anti-leishmanial agents.
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 3beta-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.
Gigante
Federica
F
University of Dundee, Sir James Black Centre, UK.
Kaiser
Marcel
M
Brun
Reto
R
Gilbert
Ian H
IH
D000818:Animals; D000981:Antiprotozoal Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D001372:Aza Compounds / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D006801:Humans; D007891:Leishmania / Q000187:drug effects*; D021261:Parasitic Sensitivity Tests; D013261:Sterols / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D014344:Trypanocidal Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D014345:Trypanosoma / Q000187:drug effects; D014352:Trypanosomiasis / Q000188:drug therapy
D000981:Antiprotozoal Agents; D001372:Aza Compounds; D013261:Sterols; D014344:Trypanocidal Agents