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恰加斯病化疗面临的挑战:针对克氏锥虫检测的药物最新情况

The challenge of Chagas' disease chemotherapy: an update of drugs assayed against Trypanosoma cruzi.

作者信息

de Castro S L

机构信息

Departamento de Ultraestrutura e Biologia Celular, Instituto Oswaldo Cruz, Fundaçào Oswaldo Cruz, Rio de Janeiro, Brazil.

出版信息

Acta Trop. 1993 Apr;53(2):83-98. doi: 10.1016/0001-706x(93)90021-3.

DOI:10.1016/0001-706x(93)90021-3
PMID:8098901
Abstract

The chemotherapy of Chagas' disease remains an unsolved problem, and the search for alternative drugs continues. Only two nitroheterocyclic drugs are in clinical use at the present time, and these have severely restricted applicability for chronic patients, as well as being highly toxic. This review covers drugs tested in the last 12 years. A large number of different compounds have been assayed in a variety of ways, most commonly in terms of their capacity to inhibit epimastigote proliferation. Allopurinol has emerged for the treatment of chronic cases. However, only with greater knowledge of the biochemistry of the parasite and in particular of its peculiarities, will it be possible to shift the emphasis of drug research away from random screenings onto a more rational footing. This is exemplified by recent studies carried out using purine derivatives and trypanothione reductase inhibitors.

摘要

恰加斯病的化疗仍是一个未解决的问题,人们仍在继续寻找替代药物。目前仅有两种硝基杂环药物在临床使用,而这些药物对慢性病患者的适用性严重受限,且毒性很高。本综述涵盖了过去12年中所测试的药物。大量不同的化合物已通过多种方式进行了检测,最常见的是根据它们抑制无鞭毛体增殖的能力来检测。别嘌呤醇已用于治疗慢性病例。然而,只有更深入了解寄生虫的生物化学,尤其是其独特之处,才有可能将药物研究的重点从随机筛选转向更合理的基础。最近使用嘌呤衍生物和锥虫硫醇还原酶抑制剂进行的研究就是例证。

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