喹啉杂化衍生物作为治疗结核病的有效结构基团：强调结构-活性关系。

IF 2.8 3区医学 Q3 IMMUNOLOGY

Tuberculosis Pub Date : 2024-11-03 DOI:10.1016/j.tube.2024.102573

Venkatraman Hegde , Raveendra Madhukar Bhat , Srinivasa Budagumpi , Vinayak Adimule , Rangappa S. Keri

{"title":"喹啉杂化衍生物作为治疗结核病的有效结构基团：强调结构-活性关系。","authors":"Venkatraman Hegde , Raveendra Madhukar Bhat , Srinivasa Budagumpi , Vinayak Adimule , Rangappa S. Keri","doi":"10.1016/j.tube.2024.102573","DOIUrl":null,"url":null,"abstract":"<div><div><em>Mycobacterium tuberculosis (MTB/Mtb)</em> is the causative agent of tuberculosis (TB), a highly infectious serious airborne illness. TB usually affects the lungs, in 25 % of patients (children or immune impaired adults), mycobacteria can enter the blood stream and infect other bodily areas such the meninges, pleura, lymphatic system, genitourinary system, bones, and joints. Currently, the most challenging aspect of treating this illness is the ineffectiveness of the most potent first-line anti-TB medications, isoniazid, rifampin, pyrazinamide, and ethambutol, which can result in multidrug-resistant TB (MDR-TB), extensively drug-resistant TB (XDR-TB), and in rare instances, completely drug-resistant TB (TDR-TB). As a result, finding new pharmaceutical compounds to treat these diseases is a significant challenge for the scientific community. A number of bio-active molecules have been investigated in this quest, including quinoline, which is considered a promising candidate for the development of TB drugs. It is known that quinoline are low in toxicity and have a wide range of pharmacological properties. Researchers have investigated quinoline scaffolds as anti-TB drugs based on their biological spectrum. The objective of this review is to examine the recent development of quinoline and its structural characteristics crucial to its antitubercular (anti-TB) activity. A molecular analog of the TB treatment can be designed and identified with this information. As a result, future generation quinoline-based anti-TB agents with greater potency and safety can also be explored.</div></div>","PeriodicalId":23383,"journal":{"name":"Tuberculosis","volume":"149 ","pages":"Article 102573"},"PeriodicalIF":2.8000,"publicationDate":"2024-11-03","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Quinoline hybrid derivatives as effective structural motifs in the treatment of tuberculosis: Emphasis on structure-activity relationships\",\"authors\":\"Venkatraman Hegde , Raveendra Madhukar Bhat , Srinivasa Budagumpi , Vinayak Adimule , Rangappa S. Keri\",\"doi\":\"10.1016/j.tube.2024.102573\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"<div><div><em>Mycobacterium tuberculosis (MTB/Mtb)</em> is the causative agent of tuberculosis (TB), a highly infectious serious airborne illness. TB usually affects the lungs, in 25 % of patients (children or immune impaired adults), mycobacteria can enter the blood stream and infect other bodily areas such the meninges, pleura, lymphatic system, genitourinary system, bones, and joints. Currently, the most challenging aspect of treating this illness is the ineffectiveness of the most potent first-line anti-TB medications, isoniazid, rifampin, pyrazinamide, and ethambutol, which can result in multidrug-resistant TB (MDR-TB), extensively drug-resistant TB (XDR-TB), and in rare instances, completely drug-resistant TB (TDR-TB). As a result, finding new pharmaceutical compounds to treat these diseases is a significant challenge for the scientific community. A number of bio-active molecules have been investigated in this quest, including quinoline, which is considered a promising candidate for the development of TB drugs. It is known that quinoline are low in toxicity and have a wide range of pharmacological properties. Researchers have investigated quinoline scaffolds as anti-TB drugs based on their biological spectrum. The objective of this review is to examine the recent development of quinoline and its structural characteristics crucial to its antitubercular (anti-TB) activity. A molecular analog of the TB treatment can be designed and identified with this information. As a result, future generation quinoline-based anti-TB agents with greater potency and safety can also be explored.</div></div>\",\"PeriodicalId\":23383,\"journal\":{\"name\":\"Tuberculosis\",\"volume\":\"149 \",\"pages\":\"Article 102573\"},\"PeriodicalIF\":2.8000,\"publicationDate\":\"2024-11-03\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Tuberculosis\",\"FirstCategoryId\":\"3\",\"ListUrlMain\":\"https://www.sciencedirect.com/science/article/pii/S1472979224000994\",\"RegionNum\":3,\"RegionCategory\":\"医学\",\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q3\",\"JCRName\":\"IMMUNOLOGY\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Tuberculosis","FirstCategoryId":"3","ListUrlMain":"https://www.sciencedirect.com/science/article/pii/S1472979224000994","RegionNum":3,"RegionCategory":"医学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q3","JCRName":"IMMUNOLOGY","Score":null,"Total":0}

引用次数: 0

摘要

结核分枝杆菌（MTB/Mtb）是肺结核（TB）的病原体，这是一种通过空气传播的高度传染性严重疾病。肺结核通常影响肺部，但 25% 的患者（儿童或免疫力低下的成年人）的分枝杆菌可进入血流并感染其他身体部位，如脑膜、胸膜、淋巴系统、泌尿生殖系统、骨骼和关节。目前，治疗这种疾病的最大挑战在于最有效的一线抗结核药物（异烟肼、利福平、吡嗪酰胺和乙胺丁醇）效果不佳，可能导致耐多药结核病（MDR-TB）、广泛耐药结核病（XDR-TB），在极少数情况下还会出现完全耐药结核病（TDR-TB）。因此，寻找治疗这些疾病的新药物化合物是科学界面临的一项重大挑战。在这一过程中，人们研究了许多生物活性分子，其中包括被认为有望开发出结核病药物的喹啉。众所周知，喹啉毒性低，具有广泛的药理特性。研究人员根据喹啉的生物谱研究了作为抗结核药物的喹啉支架。本综述旨在研究喹啉的最新发展及其对抗结核活性至关重要的结构特征。有了这些信息，就可以设计和确定治疗结核病的分子类似物。因此，还可以探索效力更强、更安全的新一代喹啉类抗结核药物。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

Quinoline hybrid derivatives as effective structural motifs in the treatment of tuberculosis: Emphasis on structure-activity relationships

查看原文本刊更多论文

Quinoline hybrid derivatives as effective structural motifs in the treatment of tuberculosis: Emphasis on structure-activity relationships

Mycobacterium tuberculosis (MTB/Mtb) is the causative agent of tuberculosis (TB), a highly infectious serious airborne illness. TB usually affects the lungs, in 25 % of patients (children or immune impaired adults), mycobacteria can enter the blood stream and infect other bodily areas such the meninges, pleura, lymphatic system, genitourinary system, bones, and joints. Currently, the most challenging aspect of treating this illness is the ineffectiveness of the most potent first-line anti-TB medications, isoniazid, rifampin, pyrazinamide, and ethambutol, which can result in multidrug-resistant TB (MDR-TB), extensively drug-resistant TB (XDR-TB), and in rare instances, completely drug-resistant TB (TDR-TB). As a result, finding new pharmaceutical compounds to treat these diseases is a significant challenge for the scientific community. A number of bio-active molecules have been investigated in this quest, including quinoline, which is considered a promising candidate for the development of TB drugs. It is known that quinoline are low in toxicity and have a wide range of pharmacological properties. Researchers have investigated quinoline scaffolds as anti-TB drugs based on their biological spectrum. The objective of this review is to examine the recent development of quinoline and its structural characteristics crucial to its antitubercular (anti-TB) activity. A molecular analog of the TB treatment can be designed and identified with this information. As a result, future generation quinoline-based anti-TB agents with greater potency and safety can also be explored.

求助全文

通过发布文献求助，成功后即可免费获取论文全文。去求助

来源期刊

Tuberculosis 医学-呼吸系统

CiteScore

4.60

自引率

3.10%

发文量

审稿时长

49 days

期刊介绍： Tuberculosis is a speciality journal focusing on basic experimental research on tuberculosis, notably on bacteriological, immunological and pathogenesis aspects of the disease. The journal publishes original research and reviews on the host response and immunology of tuberculosis and the molecular biology, genetics and physiology of the organism, however discourages submissions with a meta-analytical focus (for example, articles based on searches of published articles in public electronic databases, especially where there is lack of evidence of the personal involvement of authors in the generation of such material). We do not publish Clinical Case-Studies. Areas on which submissions are welcomed include: -Clinical TrialsDiagnostics- Antimicrobial resistance- Immunology- Leprosy- Microbiology, including microbial physiology- Molecular epidemiology- Non-tuberculous Mycobacteria- Pathogenesis- Pathology- Vaccine development. This Journal does not accept case-reports. The resurgence of interest in tuberculosis has accelerated the pace of relevant research and Tuberculosis has grown with it, as the only journal dedicated to experimental biomedical research in tuberculosis.