Universidad de Antioquia-UdeA, Calle 70 No. 52-21, A.A 1226, Medellín, Colombia, Chemistry of Colombian Plants, Institute of Chemistry, Exact and Natural Sciences School, Colombia.
Curr Med Chem. 2018;25(30):3637-3679. doi: 10.2174/0929867325666180309111428.
Leishmaniasis and Chagas disease are endemic pathologies in tropical countries. These cause high morbidity and a public health problem. Current chemotherapies are based on conventional drugs with variable efficacy and toxicity related with the length of therapeutic schemes and high doses. When two pharmacological agents are combined into a single molecule, the result is the so-called hybrid molecule. In the search for new treatments against Chagas disease and leishmaniasis, several studies have shown that hybrid molecules display high antiprotozoal activity and this emerging strategy is quite promising in the field of new drug discovery and development. This review focuses on the antiprotozoal activity of different hybrids obtained from the hybridization of pharmacophores, showing that the most of the efforts have been concentrated in the molecular hybridization of quinoline, chalcone and hydrazone moieties.
利什曼病和恰加斯病是热带国家的地方病。这些疾病导致高发病率和公共卫生问题。目前的化疗药物基于疗效不同的传统药物，与治疗方案的长度和高剂量有关，具有毒性。当两种药理制剂结合成单个分子时，其结果是所谓的杂合分子。在寻找治疗恰加斯病和利什曼病的新方法的过程中，多项研究表明，杂合分子显示出很高的抗原生动物活性，这种新兴策略在新药发现和开发领域非常有前途。这篇综述集中讨论了不同杂合子的抗原生动物活性，这些杂合子是通过药效团的杂交获得的，表明大多数努力都集中在喹啉、查耳酮和腙部分的分子杂交上。
