关键词: Anti-infective potential Antimicrobial resistance Quinolone SAR

来  源:   DOI:10.1007/s11030-024-10862-4

Abstract:
Prevalence of microbial infections and new rising pathogens are signified as causative agent for variety of serious and lethal health crisis in past years. Despite medical advances, bacterial and fungal infections continue to be a rising problem in the health care system. As more bacteria develop resistance to antibiotics used in therapy, and as more invasive microbial species develop resistance to conventional antimicrobial drugs. Relevant published publications from the last two decades, up to 2024, were systematically retrieved from the MEDLINE/PubMed, SCOPUS, EMBASE, and WOS databases using keywords such as quinolones, anti-infective, antibacterial, antimicrobial resistance and patents on quinolone derivatives. With an approach of considerable interest towards novel heterocyclic derivatives as novel anti-infective agents, researchers have explored these as essential tools in vistas of drug design and development. Among heterocycles, quinolones have been regarded extremely essential for the development of novel derivatives, even able to tackle the associated resistance issues. The quinolone scaffold with its bicyclic structure and specific functional groups such as the carbonyl and acidic groups, is indeed considered a valuable functionalities for further lead generation and optimization in drug discovery. Besides, the substitution at N-1, C-3 and C-7 positions also subjected to be having a significant role in anti-infective potential. In this article, we intend to highlight recent quinolone derivatives based on the SAR approach and anti-infective potential such as antibacterial, antifungal, antimalarial, antitubercular, antitrypanosomal and antiviral activities. Moreover, some recent patents granted on quinolone-containing derivatives as anti-infective agents have also been highlighted in tabular form. Due consideration of this, future research in this scaffold is expected to be useful for aspiring scientists to get pharmacologically significant leads.
摘要:
在过去的几年中,微生物感染和新的病原体的流行被认为是各种严重和致命的健康危机的病原体。尽管医学上有进步,细菌和真菌感染仍然是医疗保健系统中一个日益严重的问题。随着越来越多的细菌对治疗中使用的抗生素产生耐药性,并且随着更具侵入性的微生物物种对常规抗菌药物产生耐药性。过去二十年的相关出版物,直到2024年,都是从MEDLINE/PubMed系统检索的,Scopus,EMBASE,和使用诸如喹诺酮类药物之类的关键字的WOS数据库,抗感染,抗菌,喹诺酮衍生物的抗菌素耐药性和专利。随着对新型杂环衍生物作为新型抗感染剂的关注,研究人员已经将这些作为药物设计和开发的基本工具进行了探索。在杂环中,喹诺酮类药物被认为对新型衍生物的开发非常重要,甚至能够解决相关的抵抗问题。喹诺酮支架具有双环结构和特定的官能团,如羰基和酸性基团,确实被认为是在药物发现中进一步产生和优化的有价值的功能。此外,在N-1,C-3和C-7位置的取代也在抗感染潜力中具有重要作用。在这篇文章中,我们打算强调最近的喹诺酮衍生物基于SAR方法和抗感染潜力,如抗菌,抗真菌药,抗疟药,抗结核,抗锥虫和抗病毒活性。此外,最近授予的一些关于含喹诺酮衍生物作为抗感染剂的专利也以表格形式突出。适当考虑到这一点,这种支架的未来研究预计将有助于有抱负的科学家获得药理学上重要的线索。
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