期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 19, 期 11, 页码 3031-3035出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.04.060
关键词
Neglected tropical disease; Trypanosoma; Leishmania; Leishmaniasis; Trypanosomiasis; Docking simulations
资金
- University of Bologna (MLB)
- Deutsche Forschungsgemeinschaft [544]
Novel quinazoline-type compounds were designed as inhibitors of the parasite specific enzyme trypanothione reductase (TR), and their biological activities were evaluated. Some of our compounds inhibited TR, showed selectivity for TR over human glutathione reductase, and inhibited parasite growth in vitro. We propose that the quinazoline framework is a privileged structure that can be purposely modified to design novel TR inhibitors. Furthermore, the use of privileged motifs might emerge as an innovative approach to antiparasitic lead candidates. (C) 2009 Elsevier Ltd. All rights reserved.
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