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硫硒等排替代策略在开发新型抗查加斯病药物中的潜力。

Potential of sulfur-selenium isosteric replacement as a strategy for the development of new anti-chagasic drugs.

机构信息

University of Navarra, ISTUN Institute of Tropical Health, School of Pharmacy and Nutrition, Department of Pharmaceutical Technology and Chemistry, Campus Universitario, Irunlarrea 1, Pamplona 31008, Spain.

University of Navarra, ISTUN Institute of Tropical Health, School of Pharmacy and Nutrition, Department of Pharmaceutical Technology and Chemistry, Campus Universitario, Irunlarrea 1, Pamplona 31008, Spain.

出版信息

Acta Trop. 2022 Sep;233:106547. doi: 10.1016/j.actatropica.2022.106547. Epub 2022 Jun 3.

DOI:10.1016/j.actatropica.2022.106547
PMID:35667455
Abstract

Current treatment for Chagas disease is based on only two drugs: benznidazole and nifurtimox. Compounds containing sulfur (S) in their structure have shown promising results in vitro and in vivo against Trypanosoma cruzi, the parasite causing Chagas disease. Notably, some reports show that the isosteric replacement of S by selenium (Se) could be an interesting strategy for the development of new compounds for the treatment of Chagas disease. To date, the activity against T. cruzi of three Se- containing groups has been compared with their S counterparts: selenosemicarbazones, selenoquinones, and selenocyanates. More studies are needed to confirm the positive results of Se compounds. Therefore, we have investigated S compounds described in the literature tested against T. cruzi. We focused on those tested in vivo that allowed isosteric replacement to propose their Se counterparts as promising compounds for the future development of new drugs against Chagas disease.

摘要

目前对恰加斯病的治疗仅基于两种药物

苯并咪唑和硝呋替莫。结构中含有硫(S)的化合物在体外和体内对引起恰加斯病的寄生虫克氏锥虫表现出有希望的结果。值得注意的是,一些报告表明,用硒(Se)替代 S 可能是开发治疗恰加斯病的新化合物的有趣策略。迄今为止,已经比较了三种含硒基团对 T. cruzi 的活性与其 S 对应物的活性:硒代半卡巴嗪、硒代醌和硒代氰酸盐。需要更多的研究来证实 Se 化合物的阳性结果。因此,我们研究了文献中描述的针对 T. cruzi 的 S 化合物。我们专注于那些在体内进行测试的化合物,这些化合物允许进行等排替换,从而提出它们的 Se 对应物作为有前途的化合物,用于未来开发治疗恰加斯病的新药。

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