Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Alexandria University, Alexandria, 21521, Egypt; Pharmacy Program, Allied Health Department, College of Health Sciences, University of Bahrain, P.O. Box 32038, Bahrain.
Department of Pharmaceutical Chemistry, Faculty of Pharmacy, Alexandria University, Alexandria, 21521, Egypt.
Eur J Med Chem. 2018 Dec 5;160:229-244. doi: 10.1016/j.ejmech.2018.10.022. Epub 2018 Oct 11.
Leishmaniasis affects over 150 million people all over the world, especially in subtropical regions. Currently used antileishmanial synthesized drugs are associated with some drawbacks such as resistance and cytotoxicity, which hamper the chances of treatment. Furthermore, effective leishmanial vaccines are not well developed. Promising chemotherapy, either from natural or synthetic compounds, was or still is the most promising treatment. This review focuses on recent findings in drugs used for the treatment of leishmaniasis including; chemical and natural antileishmanial moieties, different potential targets, as well as various trials of vaccination development. Special emphasis has been paid to the mechanisms of the drugs, their safety and where possible, the structure-activity relationship to enable guided future drug discovery.
利什曼病影响全球超过 1.5 亿人,特别是在亚热带地区。目前使用的抗利什曼原虫合成药物存在一些缺点,如耐药性和细胞毒性,这阻碍了治疗的机会。此外,有效的利什曼原虫疫苗也没有很好的发展。有前途的化疗,无论是来自天然化合物还是合成化合物,曾经或仍然是最有前途的治疗方法。本综述重点介绍了用于治疗利什曼病的药物的最新发现,包括:化学和天然抗利什曼原虫部分、不同的潜在靶点,以及疫苗开发的各种试验。特别强调了药物的作用机制、安全性,在可能的情况下,还强调了结构-活性关系,以指导未来的药物发现。