کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1399977 | 1501231 | 2006 | 8 صفحه PDF | دانلود رایگان |
Two sterol families have been synthesized: the first one is nitrogenous sterols containing amino, N-hydroxyimino or cyano group and the second one is oxysterols such as ketosterol and hydroxysterols. These compounds were then evaluated in vitro against Leishmania donovani promastigotes and Trypanosoma brucei brucei trypomastigotes. The most active compounds against L. donovani promastigotes were 7β-aminomethylcholesterol and 7α,β-aminocholesterol (IC50 in a range from 1 to 3 μM, pentamidine: 2.8 μM). These compounds were active on intramacrophage amastigotes with IC50 of 1.3 μM. Such an activity justifies further in vivo antileishmanial evaluation. Against T. b. brucei, (24R,S)-24-hydroxy-24-methylcholesterol (MEC, 12.5 μM) was the most active compound from these series.
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Journal: European Journal of Medicinal Chemistry - Volume 41, Issue 10, October 2006, Pages 1109–1116