作者
Hasan MS Ibrahim, Mohammed I Al-Salabi, Nasser El Sabbagh, Neils B Quashie, Abdulsalam AM Alkhaldi, Roger Escale, Terry K Smith, Henri J Vial, Harry P de Koning
发表日期
2011/1/1
期刊
Journal of Antimicrobial Chemotherapy
卷号
66
期号
1
页码范围
111-125
出版商
Oxford University Press
简介
Objectives
To investigate the anti-kinetoplastid activity of choline-derived analogues with previously reported antimalarial efficacy.
Methods
From an existing choline analogue library, seven antimalarial compounds, representative of the first-, second- and third-generation analogues previously developed, were assessed for activity against Trypanosoma and Leishmania spp. Using a variety of techniques, the effects of choline analogue exposure on the parasites were documented and a preliminary investigation of their mode of action was performed.
Results
The activities of choline-derived compounds against Trypanosoma brucei and Leishmania mexicana were determined. The compounds displayed promising anti-kinetoplastid activity, particularly against T. brucei, to which 4/7 displayed submicromolar EC50 values for the wild-type strain. Low micromolar …
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HMS Ibrahim, MI Al-Salabi, N El Sabbagh, NB Quashie… - Journal of Antimicrobial Chemotherapy, 2011