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杂环 N-氧化物 - 一种有前途的抗结核、疟疾和被忽视的热带病药物。

Heterocyclic N-oxides - A Promising Class of Agents against Tuberculosis, Malaria and Neglected Tropical Diseases.

机构信息

Sao Paulo State University (UNESP), School of Pharmaceutical Sciences, Araraquara, Brazil.

São Paulo State University (UNESP), Institute of Chemistry, Araraquara, Brazil.

出版信息

Curr Pharm Des. 2018;24(12):1325-1340. doi: 10.2174/1381612824666180417122625.

Abstract

Heterocyclic N-oxides have emerged as promising agents against a number of diseases and disorders, especially infectious diseases. This review analyzes the emergence and development of this scaffold in the medicinal chemistry, focusing mainly on the discovery of new heterocyclic N-oxide compounds with potent activity against tuberculosis, malaria and neglected tropical diseases (i.e. leishmaniasis and Chagas disease). A number of heterocyclic N-oxides are described herein, nevertheless, the following chemical classes deserve to be highlighted due to a large number of reports in the literature about their promising pharmacological effects: furoxan, benzofuroxan, quinoxaline 1,4-di-N-oxide, indolone N-oxide and benzimidazole N-oxide. In order to describe those most promising compounds, we included in this review only those most biologically active heterocyclic Noxide published since 2000.

摘要

杂环 N-氧化物已成为治疗多种疾病和病症(尤其是传染病)的有前途的药物。本综述分析了该支架在药物化学中的出现和发展,主要侧重于发现具有抗结核、疟疾和被忽视的热带病(即利什曼病和恰加斯病)活性的新型杂环 N-氧化物化合物。本文描述了许多杂环 N-氧化物,但以下几类化学物质由于文献中大量关于其有前途的药理作用的报道而值得强调:呋咱、苯并呋咱、喹喔啉 1,4-二 N-氧化物、吲哚酮 N-氧化物和苯并咪唑 N-氧化物。为了描述那些最有前途的化合物,我们在综述中仅纳入了自 2000 年以来发表的最具生物活性的杂环 N-氧化物。

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