关键词: aminopyridine chagas disease drug design human african trypanosiomasis leischmaniasis neglected tropical diseases pharmacochemical properties pharmacokinetic properties

Mesh : Neglected Diseases / drug therapy Humans Antiprotozoal Agents / pharmacology chemistry chemical synthesis Trypanosoma cruzi / drug effects Aminopyridines / chemistry pharmacology Trypanosoma brucei brucei / drug effects Leishmania / drug effects Drug Development Parasitic Sensitivity Tests Animals

来  源:   DOI:10.1080/17568919.2024.2359361   PDF(Pubmed)

Abstract:
Neglected tropical diseases (NTDs) pose a major threat in tropical zones for impoverished populations. Difficulty of access, adverse effects or low efficacy limit the use of current therapeutic options. Therefore, development of new drugs against NTDs is a necessity. Compounds containing an aminopyridine (AP) moiety are of great interest for the design of new anti-NTD drugs due to their intrinsic properties compared with their closest chemical structures. Currently, over 40 compounds with an AP moiety are on the market, but none is used against NTDs despite active research on APs. The aim of this review is to present the medicinal chemistry work carried out with these scaffolds, against protozoan NTDs: Trypanosoma cruzi, Trypanosoma brucei or Leishmania spp.
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摘要:
被忽视的热带病(NTD)在热带地区对贫困人口构成了重大威胁。难以接近,副作用或低疗效限制了目前治疗方案的使用。因此,开发针对NTDs的新药是必要的。含有氨基吡啶(AP)部分的化合物由于其与其最接近的化学结构相比的固有性质而对设计新的抗NTD药物具有极大的兴趣。目前,市场上有超过40种具有AP部分的化合物,但尽管对AP进行了积极的研究,但没有一个用于NTD。这篇综述的目的是介绍使用这些支架进行的药物化学工作,对抗原生动物NTDs:克氏锥虫,布鲁氏锥虫或利什曼原虫。
[方框:见正文]。
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