Anti-Trypanosoma cruzi compounds: our contribution for the evaluation and insights on the mode of action of naphthoquinones and derivatives

Journal of the Brazilian Chemical Society

Eufrânio N. Da Silva Júnior²  Guilherme A. M. Jardim²  Rubem F. S. Menna-barreto¹  Solange L. De Castro¹ 

[1] ,Universidade Federal de Minas Gerais Instituto de Ciências Exatas Departamento de QuímicaBelo Horizonte MG ,Brazil

关键词: naphthoquinones;    β-lapachone;    Trypanosoma cruzi;    Chagas disease;    chemotherapy;   

DOI  :  10.5935/0103-5053.20140180

来源: SciELO

【 摘 要 】

Chagas disease is caused by the parasite Trypanosoma cruzi and affects approximately eight million individuals in the developing world; it is also classified as a neglected tropical disease by the World Health Organization. The available therapy for this disease is based on two nitroheterocycles, nifurtimox and benznidazole, both of which exhibit severe side effects and variable efficacy; therefore, new drugs and better treatment schedules are urgently needed. For the past 20 years, we have been collaborating with groups focused on medicinal chemistry to produce experimental therapies for Chagas disease by investigating the efficacy, selectivity, toxicity, cellular targets and mechanisms of action of different classes of compounds against T. cruzi. In this report, we present an overview of these studies, focusing on naphthoquinonoid prototypes and discuss their synthesis, activity and mechanisms of action. Furthermore, we summarise the research that has been performed to date and suggest future research directions while assessing and discussing potential improvements. This mini-review discusses our continued efforts toward the biological characterisation and synthesis of naphthoquinoidal compounds, aiming to contribute to the development of a new arsenal of candidate drugs that exhibit effective anti-T. cruzi activity

【 授权许可】

CC BY   
 All the contents of this journal, except where otherwise noted, is licensed under a Creative Commons Attribution License