Suppr超能文献

香豆素杂化物作为潜在抗HIV药物的合成、POM分析及构效关系研究的最新进展——一篇综述短文

Recent Progress in Synthesis, POM Analyses and SAR of Coumarin-Hybrids as Potential Anti-HIV Agents-A Mini Review.

作者信息

Suleiman Mustapha, Almalki Faisal A, Ben Hadda Taibi, Kawsar Sarkar M A, Chander Subhash, Murugesan Sankaranarayanan, Bhat Ajmal R, Bogoyavlenskiy Andrey, Jamalis Joazaizulfazli

机构信息

Department of Chemistry, Faculty of Science, Universiti Teknologi Malaysia, Johor Bahru 81310, Johor, Malaysia.

Department of Chemistry, Sokoto State University, Birnin Kebbi Road, Sokoto 852101, Nigeria.

出版信息

Pharmaceuticals (Basel). 2023 Oct 31;16(11):1538. doi: 10.3390/ph16111538.

Abstract

The human immunodeficiency virus (HIV) is the primary cause of acquired immune deficiency syndrome (AIDS), one of the deadliest pandemic diseases. Various mechanisms and procedures have been pursued to synthesise several anti-HIV agents, but due to the severe side effects and multidrug resistance spawning from the treatment of HIV/AIDS using highly active retroviral therapy (HAART), it has become imperative to design and synthesise novel anti-HIV agents. Literature has shown that natural sources, particularly the plant kingdom, can release important metabolites that have several biological, mechanistic and structural representations similar to chemically synthesised compounds. Certainly, compounds from natural and ethnomedicinal sources have proven to be effective in the management of HIV/AIDS with low toxicity, fewer side effects and affordability. From plants, fungi and bacteria, coumarin can be obtained, which is a secondary metabolite and is well known for its actions in different stages of the HIV replication cycle: protease, integrase and reverse transcriptase (RT) inhibition, cell membrane fusion and viral host attachment. These, among other reasons, are why coumarin moieties will be the basis of a good building block for the development of potent anti-HIV agents. This review aims to outline the synthetic pathways, structure-activity relationship (SAR) and POM analyses of coumarin hybrids with anti-HIV activity, detailing articles published between 2000 and 2023.

摘要

人类免疫缺陷病毒(HIV)是获得性免疫缺陷综合征(AIDS)的主要病因,AIDS是最致命的大流行疾病之一。人们已经采用了各种机制和程序来合成多种抗HIV药物,但由于使用高效抗逆转录病毒疗法(HAART)治疗HIV/AIDS会产生严重的副作用和多重耐药性,因此设计和合成新型抗HIV药物变得势在必行。文献表明,天然来源,特别是植物界,可以释放出重要的代谢产物,这些代谢产物具有一些与化学合成化合物相似的生物学、机制和结构特征。当然,来自天然和民族药用来源的化合物已被证明在治疗HIV/AIDS方面有效,且毒性低、副作用少、价格低廉。从植物、真菌和细菌中可以获得香豆素,它是一种次生代谢产物,以其在HIV复制周期不同阶段的作用而闻名:蛋白酶、整合酶和逆转录酶(RT)抑制、细胞膜融合和病毒与宿主的附着。基于这些以及其他原因,香豆素部分将成为开发强效抗HIV药物的良好构建基础。本综述旨在概述具有抗HIV活性的香豆素杂化物的合成途径、构效关系(SAR)和POM分析,详细介绍2000年至2023年间发表的文章。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/4086/10675815/838e61c3e7aa/pharmaceuticals-16-01538-g011.jpg

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