Suppr超能文献

氮杂环类支架的生物勘探具有潜在的忽视寄生虫病作用:综述。

Bioprospecting of Nitrogenous Heterocyclic Scaffolds with Potential Action for Neglected Parasitosis: A Review.

机构信息

Universidade Estadual da Paraiba, R. Baraunas, 351, Cidade Universitaria, Campina Grande, Paraiba, 58429-500, Brazil.

Universidade Federal de Pernambuco, Av. Prof. Moraes Rego 1235, Cidade Universitaria, Recife, Pernambuco, 50670-901, Brazil.

出版信息

Curr Pharm Des. 2020;26(33):4112-4150. doi: 10.2174/1381612826666200701160904.

Abstract

Neglected parasitic diseases are a group of infections currently considered as a worldwide concern. This fact can be attributed to the migration of these diseases to developed and developing countries, associated with therapeutic insufficiency resulted from the low investment in the research and development of new drugs. In order to overcome this situation, bioprospecting supports medicinal chemistry in the identification of new scaffolds with therapeutically appropriate physicochemical and pharmacokinetic properties. Among them, we highlight the nitrogenous heterocyclic compounds, as they are secondary metabolites of many natural products with potential biological activity. The objective of this work was to review studies within a 10-year timeframe (2009- 2019), focusing on the pharmacological application of nitrogen bioprospectives (pyrrole, pyridine, indole, quinoline, acridine, and their respective derivatives) against neglected parasitic infections (malaria, leishmania, trypanosomiases, and schistosomiasis), and their application as a template for semi-synthesis or total synthesis of potential antiparasitic agents. In our studies, it was observed that among the selected articles, there was a higher focus on the attempt to identify and obtain novel antimalarial compounds, in a way that an extensive amount of studies involving all heterocyclic nitrogen nuclei were found. On the other hand, the parasites with the lowest number of publications up until the present date have been trypanosomiasis, especially those caused by Trypanosoma cruzi, and schistosomiasis, where some heterocyclics have not even been cited in recent years. Thus, we conclude that despite the great biodiversity on the planet, little attention has been given to certain neglected tropical diseases, especially those that reach countries with a high poverty rate.

摘要

被忽视的寄生虫病是一组目前被认为是全球关注的传染病。这一事实可以归因于这些疾病向发达国家和发展中国家的迁移,以及由于对新药研发的投资不足而导致的治疗不足。为了克服这种情况,生物勘探支持药物化学识别具有治疗适当的物理化学和药代动力学特性的新骨架。其中,我们强调含氮杂环化合物,因为它们是许多具有潜在生物活性的天然产物的次生代谢物。这项工作的目的是回顾在 10 年时间范围内(2009-2019 年)的研究,重点关注氮生物勘探(吡咯、吡啶、吲哚、喹啉、吖啶及其各自的衍生物)在治疗被忽视的寄生虫感染(疟疾、利什曼病、锥虫病和血吸虫病)方面的药理学应用,以及它们作为潜在抗寄生虫药物的半合成或全合成模板的应用。在我们的研究中,观察到在所选择的文章中,更多地关注试图识别和获得新型抗疟化合物,以至于发现了大量涉及所有杂环氮核的研究。另一方面,到目前为止,出版物数量最少的寄生虫病是锥虫病,特别是由克氏锥虫引起的锥虫病,近年来甚至没有引用过一些杂环化合物。因此,我们得出结论,尽管地球上有巨大的生物多样性,但对某些被忽视的热带病关注甚少,特别是那些达到高贫困率国家的疾病。

文献检索

告别复杂PubMed语法,用中文像聊天一样搜索,搜遍4000万医学文献。AI智能推荐,让科研检索更轻松。

立即免费搜索

文件翻译

保留排版,准确专业,支持PDF/Word/PPT等文件格式,支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述,25分钟生成高质量综述,智能提取关键信息,辅助科研写作。

立即免费体验