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氨基吡啶类化合物在抗原虫性热带病药物研发中的应用。

Aminopyridines in the development of drug candidates against protozoan neglected tropical diseases.

机构信息

Université de Picardie-Jules-Verne, AGIR - Agents infectieux, RéSistance et chimiothérapie, UR 4294, UFR de pharmacie, 1, Rue des Louvels, F-80037 Amiens cedex 1, France.

出版信息

Future Med Chem. 2024 Jul 2;16(13):1357-1373. doi: 10.1080/17568919.2024.2359361. Epub 2024 Jun 10.

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: , or .

摘要

被忽视的热带病(NTDs)对贫困地区的热带人群构成重大威胁。由于目前治疗方案存在获取困难、不良反应或疗效低下等问题,限制了其使用。因此,开发针对 NTDs 的新药是必要的。含氨基吡啶(AP)部分的化合物因其与最接近的化学结构相比具有内在特性,因此非常适合用于设计新型抗 NTD 药物。目前,市场上有超过 40 种含 AP 部分的化合物,但没有一种用于治疗 NTDs,尽管人们对 AP 进行了积极的研究。本文综述了针对原生动物 NTDs(即利什曼原虫、锥虫或疟原虫)的这些支架的药物化学研究工作。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b059/11318709/ff44df0b9ad1/IFMC_A_2359361_UF0001_C.jpg

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