富马酸clemastine类似物作为有效抗利什曼动物。

IF 3.597 Q2 Pharmacology, Toxicology and Pharmaceutics
MedChemComm Pub Date : 2025-01-31 DOI:10.1039/D4MD01004C
Rebecca L. Charlton, Douglas O. Escrivani, Christopher Brown, Niranjan Thota, Victor S. Agostino, Exequiel O. J. Porta, Timur Avkiran, Andrew T. Merritt, Paul W. Denny, Bartira Rossi-Bergmann and Patrick G. Steel
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引用次数: 0

摘要

目前利什曼病的治疗方案严重有限,这突出表明迫切需要开发更有效和毒性更小的药物,以应对一项重大的全球公共卫生挑战。Clemastine延胡索酸酯显示良好水平的antileishmanial功效,但进一步优化合成挑战的困难。在这里,我们证明了简单的n链类似物更容易获得,可以表现出更高的选择性,并在亚马逊利什曼原虫感染的小鼠模型中显示出相当的功效。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Simple accessible clemastine fumarate analogues as effective antileishmanials†

Current therapeutic options for leishmaniasis are severely limited, highlighting an urgent need to develop more effective and less toxic drugs to combat a major global public health challenge. Clemastine fumarate displays good levels of antileishmanial efficacy, but further optimisation is challenged by its difficult synthesis. Here, we demonstrate that simple N-linked analogues are easier to access, can exhibit higher selectivity and show comparable efficacy in a mouse model of Leishmania amazonensis infection.

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来源期刊
MedChemComm
MedChemComm BIOCHEMISTRY & MOLECULAR BIOLOGY-CHEMISTRY, MEDICINAL
CiteScore
4.70
自引率
0.00%
发文量
0
审稿时长
2.2 months
期刊介绍: Research and review articles in medicinal chemistry and related drug discovery science; the official journal of the European Federation for Medicinal Chemistry. In 2020, MedChemComm will change its name to RSC Medicinal Chemistry. Issue 12, 2019 will be the last issue as MedChemComm.
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