Department of Medicinal Chemistry, School of Pharmacy, Ardabil University of Medical Sciences, PO Box 5618953141, Ardabil, Iran.
Department of Medicinal Chemistry, School of Pharmacy, Hamadan University of Medical Sciences, Hamadan, Iran.
Mol Divers. 2020 May;24(2):525-569. doi: 10.1007/s11030-019-09953-4. Epub 2019 Apr 26.
Leishmania, one of the most important neglected tropical diseases, is endemic in several regions of the world and hence regarded as a serious threat to public health. Major difficulties with current chemotherapeutic agents raise issues such as toxicity, resistance, cost and other side effects. These issues necessitate development of potentially new chemical entities against diverse leishmanial species. Numerous natural and synthetic new antileishmanial molecules have been described for disease management. Careful inspection of scientific reports revealed that considerable amount of promising antileishmanial agents belonged to the nitrogen-containing heterocycles such as quinoline, triazole, pyrazole, imidazole, indole, pyrimidine, β-carboline, quinoxaline, quinazoline and benzimidazole. In this regard, enormous chemical data provide the opportunity for systematic elucidation of structural requirements against different leishmanial species. Within this representation, insights into the current status of privileged N-heterocycles as antileishmanial agents with particular emphasis on structure activity relationships are reviewed.
利什曼原虫是最重要的被忽视热带病之一，在世界上的几个地区流行，因此被认为是对公共卫生的严重威胁。目前化疗药物存在毒性、耐药性、成本和其他副作用等主要问题。这些问题需要针对不同的利什曼原虫物种开发潜在的新化学实体。已经有许多天然和合成的新型抗利什曼原虫分子被用于疾病管理。仔细检查科学报告发现，相当数量有前途的抗利什曼原虫药物属于含氮杂环，如喹啉、三唑、吡唑、咪唑、吲哚、嘧啶、β-咔啉、喹喔啉、喹唑啉和苯并咪唑。在这方面，大量的化学数据为针对不同利什曼原虫物种的系统阐明结构要求提供了机会。在这种表示形式中，审查了作为抗利什曼原虫药物的特权 N-杂环的现状，特别强调了结构活性关系。
