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最近有关具有抗利什曼原虫活性的新型合成手性化合物的最新进展。

A recent update on new synthetic chiral compounds with antileishmanial activity.

机构信息

Department of Biomolecular Science, University of Urbino Carlo Bo, Urbino, Italy.

出版信息

Chirality. 2022 Oct;34(10):1279-1297. doi: 10.1002/chir.23494. Epub 2022 Aug 10.

Abstract

Parasitic diseases, including malaria, leishmaniasis, and trypanosomiasis, affect billions of people and are responsible for almost 500,000 deaths/year. In particular, leishmaniasis, a neglected tropical disease, is considered a global public health problem because current drugs have several drawbacks including to toxicity, high cost, and drug resistance, which result in a lack of effective and readily available therapies. Therefore, the synthesis of new, safe, and effective molecules still requires the attention of the scientific community. Moreover, it is well known that chirality plays a crucial role in the antiparasitic activity of molecules, driving the design of their synthesis. Therefore, in this review we report a recent update on new chiral compounds with promising antileishmanial activity, focusing on synthetic approaches. Where reported, in most cases the enantiopure compound has shown better potency against the protozoa than its enantiomer or corresponding racemic mixture.

摘要

寄生虫病,包括疟疾、利什曼病和锥虫病,影响着数十亿人,每年导致近 50 万人死亡。特别是利什曼病,作为一种被忽视的热带病,被认为是一个全球性的公共卫生问题,因为现有的药物存在多种缺点,包括毒性、高成本和耐药性,这导致缺乏有效和现成的治疗方法。因此,新的、安全和有效的分子的合成仍然需要科学界的关注。此外,众所周知,手性在分子的抗寄生虫活性中起着至关重要的作用,这推动了它们的合成设计。因此,在这篇综述中,我们报告了具有有前景的抗利什曼活性的新手性化合物的最新进展,重点介绍了合成方法。在有报道的情况下,在大多数情况下,对原生动物而言,手性纯化合物的活性优于其对映异构体或相应的外消旋混合物。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/fe29/9543214/db51c0ccae64/CHIR-34-1279-g015.jpg

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