Laboratorio de Síntese Organica Medicinal (LaSOM), Programa de Pos-Graduacao em Ciencias Farmaceuticas, Faculdade de Farmacia, Universidade Federal do Rio Grande do Sul, Porto Alegre/RS, Brazil.
Grupo de Quimica Medicinal, Laboratorio de Quimica Organica, Facultad de Ciencias, Universidad de la Republica, Montevideo, Uruguay.
Mini Rev Med Chem. 2021;21(13):1701-1717. doi: 10.2174/1389557521666201229125931.
The complexity of Chagas disease is still a challenge in endemic regions and an emergent public health problem in non-endemic countries. The causative agent of this neglected tropical disease, Trypanosoma cruzi, is mainly transmitted by triatomine vectors and possesses multiple epidemiologically important strains. Current chemotherapeutics are outdated and their limited efficacy is one of the major reasons for treatment discontinuation. In this context, the development of novel, safe and economically accessible antichagasic drugs is required. Various classes of heterocycles and natural compounds have been described as potential antichagasic scaffolds, and coumarins are no exception. These versatile compounds have a wide spectrum of biological activities, and numerous natural and synthetic coumarins have been reported with antichagasic potential. This review aims to discuss the available literature between 2001 and 2020 regarding natural and synthetic coumarins with anti- Trypanosoma cruzi activity. Moreover, some of the studies herein comprised are dedicated to the potential of coumarins to inhibit promising targets in Trypanosoma cruzi.
恰加斯病的复杂性在流行地区仍然是一个挑战,在非流行国家也是一个新出现的公共卫生问题。这种被忽视的热带病的病原体克氏锥虫主要通过锥蝽媒介传播,具有多种具有流行病学重要意义的株系。目前的化学疗法已经过时,其有限的疗效是治疗中断的主要原因之一。在这种情况下,需要开发新型、安全和经济上可获得的抗恰加斯病药物。各种杂环和天然化合物已被描述为潜在的抗恰加斯病支架,香豆素也不例外。这些多功能化合物具有广泛的生物活性,已有大量天然和合成香豆素具有抗克氏锥虫的潜力。本综述旨在讨论 2001 年至 2020 年间关于具有抗克氏锥虫活性的天然和合成香豆素的现有文献。此外,本文中的一些研究致力于香豆素抑制克氏锥虫有希望的靶标的潜力。