Owais Mohammad, Kumar Arun, Hasan Syed Misbahul, Singh Kuldeep, Azad Iqbal, Hussain Arshad, Akil Mohd
Faculty of Pharmacy, Integral University, Kursi Road, Lucknow 226026 (U.P.), India.
Department of Chemistry, Integral University, Kursi Road, Lucknow 226026 (U.P.), India.
Mini Rev Med Chem. 2024;24(13):1238-1251. doi: 10.2174/0113895575281039231218112953.
Heterocyclic compounds and their derivatives play a significant role in the design and development of novel quinoline drugs. Among the various pharmacologically active heterocyclic compounds, quinolines stand out as the most significant rings due to their broad pharmacological roles, specifically antitubercular activity, and their presence in plant-based compounds. Quinoline is also known as benzpyridine, benzopyridine, and 1-azanaphthalene. It has a benzene ring fused with a pyridine ring, and both rings share two carbon atoms. The importance of quinoline lies in its incorporation as a key component in various natural compounds found in medicinal plant families like , and others.
This article is expected to have a significant impact on the advancement of effective antitubercular drugs. Through harnessing the potent activity of quinoline derivatives, the research aims to make valuable contributions to combating tuberculosis more efficiently and ultimately reducing the global burden of this infectious disease.
Numerous nitrogen-containing heterocyclic compounds exhibit significant potential as antitubercular agents. These chemicals have fused aromatic nitrogen-heterocyclic nuclei that can change the number of electrons they have, which can change their chemical, physical, and biological properties. This versatility comes from their ability to bind with the receptors in multiple modes, a critical aspect of drug pharmacological screening. Among these compounds, quinoline stands out as it incorporates a stable fusion of a benzene ring with a pyridine nucleus. Quinolines have demonstrated a diverse range of pharmacological activities, including but not limited to anti-tubercular, anti-tumor, anticoagulant, anti-inflammatory, antioxidant, antiviral, antimalarial, anti-HIV, and antimicrobial effects.
Some molecules, such as lone-paired nitrogen species, include pyrrole, pyrazole, and quinoline. These molecules contain nitrogen and take part in metabolic reactions with other molecules inside the cell. However, an excessive accumulation of reactive nitrogen species can lead to cytotoxicity, resulting in damage to essential biological macromolecules. Among these compounds, quinoline stands out as the oldest and most effective one, exhibiting a wide range of significant properties such as antitubercular, antimicrobial, anti-inflammatory, antioxidant, analgesic, and anticonvulsant activities. Notably, naturally occurring quinoline compounds, such as quinine, have proven to be potent antimalarial drugs.
This review highlights quinoline derivatives' antitubercular potential, emphasizing recent research advancements. Utilizing IC values, the study emphasizes the efficacy of various quinoline substitutions, hybrids, and electron-withdrawing groups against . Continued research is essential for developing potent, low-toxicity quinoline derivatives to combat tuberculosis.
杂环化合物及其衍生物在新型喹啉类药物的设计与开发中发挥着重要作用。在各种具有药理活性的杂环化合物中,喹啉因其广泛的药理作用,特别是抗结核活性以及在植物性化合物中的存在,而成为最重要的环系。喹啉也被称为苯并吡啶、氮杂萘。它有一个与吡啶环稠合的苯环,两个环共用两个碳原子。喹啉的重要性在于它作为关键成分存在于诸如等药用植物科中发现的各种天然化合物中。
本文有望对有效抗结核药物的发展产生重大影响。通过利用喹啉衍生物的强大活性,该研究旨在为更有效地抗击结核病并最终减轻这种传染病的全球负担做出有价值的贡献。
许多含氮杂环化合物作为抗结核药物具有巨大潜力。这些化学物质具有稠合的芳族氮杂环核,可改变其电子数量,进而改变其化学、物理和生物学性质。这种多功能性源于它们能够以多种模式与受体结合,这是药物药理筛选的关键方面。在这些化合物中,喹啉脱颖而出,因为它包含一个苯环与吡啶核的稳定稠合。喹啉已显示出多种药理活性,包括但不限于抗结核、抗肿瘤、抗凝血、抗炎、抗氧化、抗病毒、抗疟疾、抗艾滋病毒和抗菌作用。
一些分子,如孤对氮物种,包括吡咯、吡唑和喹啉。这些分子含有氮并参与细胞内与其他分子的代谢反应。然而,活性氮物种的过度积累会导致细胞毒性,从而对重要的生物大分子造成损害。在这些化合物中,喹啉是最古老且最有效的一种,具有广泛的显著特性,如抗结核、抗菌、抗炎、抗氧化、镇痛和抗惊厥活性。值得注意的是,天然存在的喹啉化合物,如奎宁,已被证明是有效的抗疟药物。
本综述强调了喹啉衍生物的抗结核潜力,重点介绍了近期的研究进展。利用IC值,该研究强调了各种喹啉取代物、杂化物和吸电子基团对的疗效。持续研究对于开发有效的低毒喹啉衍生物以抗击结核病至关重要。