Laboratório de Síntese Orgânica Medicinal (LaSOM), Programa de Pós-Graduação Em Ciências Farmacêuticas, Faculdade de Farmácia, Universidade Federal Do Rio Grande Do Sul, 90610-000, Porto Alegre, RS, Brazil.
Laboratório de Síntese Orgânica Medicinal (LaSOM), Programa de Pós-Graduação Em Ciências Farmacêuticas, Faculdade de Farmácia, Universidade Federal Do Rio Grande Do Sul, 90610-000, Porto Alegre, RS, Brazil.
Eur J Med Chem. 2020 Oct 1;203:112514. doi: 10.1016/j.ejmech.2020.112514. Epub 2020 Jul 9.
The neglected tropical disease leishmaniasis is still a major public health problem that affects millions of people worldwide. Related to poor-living conditions, this vector-borne disease presents multiple clinical manifestations - from asymptomatic to systemic conditions. The protozoans of the genus Leishmania are the etiologic agents transmitted through the bite of sandflies, the main vectors. Current pharmacological interventions are outdated and present several drawbacks, thus the search for new antileishmanial compounds is imperative. Medicinal chemists have been continuously investigating for new alternatives to combat leishmaniasis, and coumarins play a pivotal role in this search. Various biological properties have been described owing to coumarin's structural versatility combined with its unique features, including antileishmanial activity. The aim of this review is to highlight the most relevant studies between 1997 and 2020 and provide a guide for the development of new antileishmanial coumarins. Naturally occurring and synthetically designed coumarins are comprised in this review, along with a structure-activity relationship to provide an insight for further development of coumarins with antileishmanial activity.
被忽视的热带病利什曼病仍然是一个主要的公共卫生问题，影响着全球数百万人。这种由病媒传播的疾病与恶劣的生活条件有关，表现出多种临床表现-从无症状到全身疾病。利什曼原虫属的原生动物是通过沙蝇叮咬传播的病原体，沙蝇是主要病媒。目前的药物干预措施已经过时，存在许多缺点，因此寻找新的抗利什曼病化合物势在必行。药物化学家一直在不断研究新的替代品来对抗利什曼病，香豆素在这方面的研究中起着关键作用。由于香豆素结构的多功能性及其独特的特性，包括抗利什曼活性，已经描述了各种生物学特性。本综述的目的是重点介绍 1997 年至 2020 年期间最相关的研究，并为开发新的抗利什曼香豆素提供指导。本综述包括天然存在和合成设计的香豆素，以及构效关系，为进一步开发具有抗利什曼活性的香豆素提供了深入了解。
