Abstract
The recent highlights on the biochemical pathways of Trypanosoma cruzi have allowed a significant improvement in the development of new strategies for drug design and also in the understanding of the mechanisms of action of new trypanocidal agents. Several biochemical pathways of fundamental importance and validated targets (e.g. cysteine protease cruzain, trypanothione reductase, trans-sialidase) of T. cruzi have proved usefulness for drug development in many examples of new candidates to anti-T. cruzi drugs. This review will focus on some approaches used for the design of new potential trypanocidal agents, exploring modern concepts of medicinal chemistry such as bioisosterism, molecular hybridization, bioinspired design in lead compounds, as well as the complexation of transition metals with bioactive ligands. The examples discussed in this article may serve as lessons for the antitrypanosomal drug design.
Keywords: Chagas' disease, chemotherapy, rational drug design, medicinal chemistry, Trypanosoma cruzi
Current Drug Targets
Title: Approaches for the Development of New Anti-Trypanosoma cruzi Agents
Volume: 10 Issue: 3
Author(s): Diogo Rodrigo Magalhaes Moreira, Ana Cristina Lima Leite, Ricardo Ribeiro dos Santos and Milena B. P. Soares
Affiliation:
Keywords: Chagas' disease, chemotherapy, rational drug design, medicinal chemistry, Trypanosoma cruzi
Abstract: The recent highlights on the biochemical pathways of Trypanosoma cruzi have allowed a significant improvement in the development of new strategies for drug design and also in the understanding of the mechanisms of action of new trypanocidal agents. Several biochemical pathways of fundamental importance and validated targets (e.g. cysteine protease cruzain, trypanothione reductase, trans-sialidase) of T. cruzi have proved usefulness for drug development in many examples of new candidates to anti-T. cruzi drugs. This review will focus on some approaches used for the design of new potential trypanocidal agents, exploring modern concepts of medicinal chemistry such as bioisosterism, molecular hybridization, bioinspired design in lead compounds, as well as the complexation of transition metals with bioactive ligands. The examples discussed in this article may serve as lessons for the antitrypanosomal drug design.
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Magalhaes Moreira Diogo Rodrigo, Lima Leite Cristina Ana, Santos dos Ricardo Ribeiro and Soares B. P. Milena, Approaches for the Development of New Anti-Trypanosoma cruzi Agents, Current Drug Targets 2009; 10 (3) . https://dx.doi.org/10.2174/138945009787581140
DOI https://dx.doi.org/10.2174/138945009787581140 |
Print ISSN 1389-4501 |
Publisher Name Bentham Science Publisher |
Online ISSN 1873-5592 |
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