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Natural and synthetic coumarins as antileishmanial agents: A review.
European Journal of Medicinal Chemistry ( IF 6.0 ) Pub Date : 2020-07-09 , DOI: 10.1016/j.ejmech.2020.112514
Guilherme Arraché Gonçalves 1 , Adriano Ronchi Spillere 1 , Gustavo Machado das Neves 1 , Luciano Porto Kagami 1 , Gilsane Lino von Poser 2 , Rômulo Faria Santos Canto 3 , VeraLucia Eifler-Lima 1
Affiliation  

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 Current pharmacological interventions are outdated and present several drawbacks, thus the search for new antileishmanial compounds is imperative.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.



中文翻译:

天然和合成香豆素作为抗衰老剂:综述。

被忽视的热带病利什曼病仍然是一个重大的公共卫生问题,影响着全球数百万人。与生活条件差有关,这种媒介传播的疾病表现出多种临床表现-从无症状到全身性疾病。利什曼原虫属的原生动物是通过沙蝇叮咬传播的病原体,它们是主要媒介。当前的药理学干预已经过时并且存在一些缺点,因此必须寻找新的抗兽药化合物。药物化学家一直在不断研究寻找新的替代方法来对抗利什曼病,而香豆素在该研究中起着举足轻重的作用。由于香豆素的结构多功能性及其独特的特征(包括抗猪粪活性),已描述了多种生物学特性。这篇综述的目的是突出1997年至2020年之间最相关的研究,并为新的无臭香豆素的开发提供指导。本评论包括天然存在的和合成设计的香豆素,

更新日期:2020-07-13
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