Del Carpio Edgar, Hernández Lino, Lubes Vito, Jourdan Francisco, Cerecetto Hugo, Scalese Gonzalo, Gambino Dinorah, Romero Angel H
Unidad de Química Medicinal, Facultad de Farmacia, Escuela "Dr. Jesús María Bianco", Universidad Central de Venezuela (UCV), Caracas, Venezuela.
Departamento de Química, Universidad Simón Bolívar (USB), Caracas, Venezuela.
Front Chem. 2025 May 30;13:1586044. doi: 10.3389/fchem.2025.1586044. eCollection 2025.
The quinoline moiety represents an important scaffold for the development of leishmanicidal agents. In particular, its hybridization with metal/metalloids has generated highly active compounds that are, in some cases, highly selective against leishmaniasis models. The existing leishmanicidal metal-/metalloid-quinoline compounds are mainly based on the following: (i) coordination compounds based on 8-hydroxyquinolinate; (ii) metallocene derivatives; (iii) -heterocyclic carbene (NHC) complexes featuring a quinoline moiety. This mini-review summarizes the reported cases of leishmanicidal metal and metalloid-based quinoline compounds for each group (i-iii), focusing on the structure-property relationship from models and mechanisms of action, experiments, and pharmacokinetic data, if available. This paper aims to describe the state of the art of inorganic medicinal chemistry for the development of selective and potent leishmanicidal agents using the quinoline moiety.
喹啉部分是开发抗利什曼原虫药物的重要骨架。特别是，它与金属/类金属的杂化产生了高活性化合物，在某些情况下，这些化合物对利什曼病模型具有高度选择性。现有的抗利什曼原虫金属/类金属喹啉化合物主要基于以下几类：（i）基于8-羟基喹啉酸酯的配位化合物；（ii）茂金属衍生物；（iii）具有喹啉部分的N-杂环卡宾（NHC）配合物。本综述总结了每组（i-iii）中已报道的基于金属和类金属的喹啉抗利什曼原虫化合物的案例，重点关注从作用模型和机制、实验以及药代动力学数据（如可用）方面的结构-性质关系。本文旨在描述利用喹啉部分开发选择性和强效抗利什曼原虫药物的无机药物化学的现状。
