A systematic review on the anti-microbial activities and structure-activity relationship (SAR) of quinoxaline derivatives

IF 5.9 2区 医学 Q1 CHEMISTRY, MEDICINAL European Journal of Medicinal Chemistry Pub Date : 2025-05-05 Epub Date: 2025-03-03 DOI:10.1016/j.ejmech.2025.117472
Sri Mounika Bellapukonda, Rani Bandela, Anuradha Singampalli, Danaboina Srikanth, Pardeep Kumar, Srinivas Nanduri, Venkata Madhavi Yaddanapudi
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Abstract

Anti-microbial resistance has become a serious global health issue affecting millions of people worldwide. Despite extensive drug discovery efforts aimed at identifying potent molecules for effective anti-microbial treatments, the emergence of superbugs remains a significant challenge. Thus, developing novel therapeutic agents is required to combat these evolving threats. The quinoxaline scaffold emerges as a promising heterocyclic framework for developing novel anti-microbial agents. It's simple, flexible structure, coupled with its bioisosteric relationship to extensively explored quinoline and naphthalene scaffolds, offers a potential avenue for circumventing bacterial resistance developed against these established classes. Hence it has sparked interest in researchers to develop novel antibiotics based on the quinoxaline core. This review focuses on the recent advances of quinoxaline derivatives as anti-microbial agents and their structure-activity relationship studies based on the literature published from 2015 to 2024. The systematic presentation of this information will assist researchers in identifying key substitution patterns around the quinoxaline nucleus, facilitating the development of structure-activity relationship (SAR), and guiding the design of novel anti-microbial drugs to combat the growing threat of anti-microbial resistance.

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喹诺啉类衍生物的抑菌活性及构效关系综述
抗微生物药物耐药性已成为影响全世界数百万人的严重全球健康问题。尽管广泛的药物发现努力旨在确定有效的抗微生物治疗的有效分子,超级细菌的出现仍然是一个重大的挑战。因此,需要开发新的治疗药物来对抗这些不断演变的威胁。喹诺啉支架是一种很有前途的杂环框架,可用于开发新型抗微生物药物。它简单、灵活的结构,加上它与广泛探索的喹啉和萘支架的生物等构关系,为避免细菌对这些已建立的类别产生耐药性提供了潜在的途径。因此,它激发了研究人员开发基于喹诺啉核心的新型抗生素的兴趣。本文根据2015-2024年喹诺啉类抗菌药物的相关文献,综述了喹诺啉类抗菌药物的研究进展及其构效关系。这些信息的系统呈现将有助于研究人员识别喹诺啉核周围的关键取代模式,促进构效关系(SAR)的发展,并指导新型抗微生物药物的设计,以对抗日益增长的抗微生物耐药性威胁。
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来源期刊
CiteScore
11.70
自引率
9.00%
发文量
863
审稿时长
29 days
期刊介绍: The European Journal of Medicinal Chemistry is a global journal that publishes studies on all aspects of medicinal chemistry. It provides a medium for publication of original papers and also welcomes critical review papers. A typical paper would report on the organic synthesis, characterization and pharmacological evaluation of compounds. Other topics of interest are drug design, QSAR, molecular modeling, drug-receptor interactions, molecular aspects of drug metabolism, prodrug synthesis and drug targeting. The journal expects manuscripts to present the rational for a study, provide insight into the design of compounds or understanding of mechanism, or clarify the targets.
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