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吲哚及其相关杂化物抗感染潜力的最新进展洞察

An insight into the recent developments in anti-infective potential of indole and associated hybrids.

作者信息

Mathada Basavarajaiah Suliphuldevara, Somappa Sasidhar B

机构信息

Post Graduate Department of Chemistry, Vijaya College, Bengaluru, Karnataka 560 004, India.

Organic Chemistry Section, Chemical Sciences and Technology Division, CSIR-National Institute for Interdisciplinary Science and Technology (NIIST), Thiruvananthapuram 695 019, India.

出版信息

J Mol Struct. 2022 Aug 5;1261:132808. doi: 10.1016/j.molstruc.2022.132808. Epub 2022 Mar 11.

Abstract

Prevention, accurate diagnosis, and effective treatment of infections are the main challenges in the overall management of infectious diseases. The best example is the ongoing SARs-COV-2(COVID-19) pandemic; the entire world is extremely worried about at present. Interestingly, heterocyclic moieties provide an ideal scaffold on which suitable pharmacophores can be designed to construct novel drugs. Indoles are amongst the most essential class of heteroaromatics in medicinal chemistry, which are ubiquitous across natural sources. The aforesaid derivatives have become invaluable scaffolds because of their wide spectrum therapeutic applications. Therefore, many researchers are focused on the design and synthesis of indole and associated hybrids of biological relevance. Hence, in the present review, we concisely discuss the indole containing natural sources, marketed drugs, clinical candidates, and their biological activities like antibacterial, antifungal, anti-TB, antiviral, antimalarial, and anti-leishmanial activities. The structure-activity relationships study of indole derivatives is also presented for a better understanding of the identified structures. The literature data presented for the anti-infective agents herein covers largely for the last twelve years.

摘要

感染的预防、准确诊断和有效治疗是传染病整体管理中的主要挑战。最好的例子就是当前正在肆虐的严重急性呼吸综合征冠状病毒2(SARS-CoV-2,即新冠病毒)疫情,这是目前全世界极为担忧的事情。有趣的是,杂环部分提供了一个理想的骨架,在其上可以设计合适的药效基团来构建新型药物。吲哚是药物化学中最重要的杂芳烃类别之一,广泛存在于天然来源中。由于上述衍生物具有广泛的治疗应用,它们已成为非常有价值的骨架。因此,许多研究人员专注于设计和合成具有生物学相关性的吲哚及其相关杂化物。因此,在本综述中,我们简要讨论了含吲哚的天然来源、上市药物、临床候选药物及其抗菌、抗真菌、抗结核、抗病毒、抗疟疾和抗利什曼原虫等生物活性。还介绍了吲哚衍生物的构效关系研究,以便更好地理解所确定的结构。本文中关于抗感染药物的文献数据主要涵盖过去十二年。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/da3b/8913251/8146a75099ee/ga1_lrg.jpg

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