Exploration of triazole derivatives, SAR profiles, and clinical pipeline against Mycobacterium tuberculosis

IF 4.5 2区医学 Q1 BIOCHEMISTRY & MOLECULAR BIOLOGY

Bioorganic Chemistry Pub Date : 2025-02-01 DOI:10.1016/j.bioorg.2024.108114

Kakarla Pakeeraiah , Krishna Kartheek Chinchilli , Rambabu Dandela , Sudhir Kumar Paidesetty

引用次数: 0

Abstract

Tuberculosis is a highly infectious disease and it is a global threat in particular affecting people from developing countries. It is thought that nearly one-third of the global population lives with this causative bacterium in its dominant form. The spread of HIV and the development of resistance to both multidrug-resistant TB (MDR-TB) and extensively drug-resistant TB (XDR-TB) aggravates the spread of the disease and needs novel drugs which combat this disease effectively. Triazole-containing anti-tubercular drugs are promising and need further tuning to develop as a potent scaffold for tuberculosis. In this review, we highlight the structural activity relationships of triazole-containing drugs and detailed understanding for the researchers in the field of medicinal chemistry to further explore these triazole-based compounds as well as synthesize new compounds for antitubercular activity against drug-sensitive and resistant strains.

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抗结核分枝杆菌的三唑衍生物、SAR谱和临床管道的探索。

结核病是一种传染性很强的疾病，是一种全球威胁，尤其影响到发展中国家的人民。据认为，全球近三分之一的人口携带这种主要形式的致病细菌。艾滋病毒的传播以及对耐多药结核病（MDR-TB）和广泛耐药结核病（XDR-TB）的耐药性的发展加剧了该疾病的传播，需要有效防治该疾病的新药。含三氮唑的抗结核药物很有前景，需要进一步调整以发展成为一种有效的结核病支架。本文综述了含三唑类药物的结构与活性关系，为药物化学领域的研究人员进一步探索这些基于三唑类药物的化合物以及合成具有抗药敏和耐药活性的新化合物提供了详细的认识。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Bioorganic Chemistry 生物-生化与分子生物学

CiteScore

9.70

自引率

3.90%

发文量

679

审稿时长

31 days

期刊介绍： Bioorganic Chemistry publishes research that addresses biological questions at the molecular level, using organic chemistry and principles of physical organic chemistry. The scope of the journal covers a range of topics at the organic chemistry-biology interface, including: enzyme catalysis, biotransformation and enzyme inhibition; nucleic acids chemistry; medicinal chemistry; natural product chemistry, natural product synthesis and natural product biosynthesis; antimicrobial agents; lipid and peptide chemistry; biophysical chemistry; biological probes; bio-orthogonal chemistry and biomimetic chemistry. For manuscripts dealing with synthetic bioactive compounds, the Journal requires that the molecular target of the compounds described must be known, and must be demonstrated experimentally in the manuscript. For studies involving natural products, if the molecular target is unknown, some data beyond simple cell-based toxicity studies to provide insight into the mechanism of action is required. Studies supported by molecular docking are welcome, but must be supported by experimental data. The Journal does not consider manuscripts that are purely theoretical or computational in nature. The Journal publishes regular articles, short communications and reviews. Reviews are normally invited by Editors or Editorial Board members. Authors of unsolicited reviews should first contact an Editor or Editorial Board member to determine whether the proposed article is within the scope of the Journal.