Sharma Vishal, Saini Monika, Das Rina, Chauhan Samrat, Sharma Diksha, Mujwar Somdutt, Gupta Sumeet, Mehta Dinesh Kumar
Department of Pharmaceutical Chemistry, MM College of Pharmacy, Maharishi Markandeshwar (Deemed to be University), Ambala, India.
Department of Pharmacology, Chitkara College of Pharmacy, Chitkara University, Rajpura, Punjab, India.
Chem Biodivers. 2025 May;22(5):e202401936. doi: 10.1002/cbdv.202401936. Epub 2025 Jan 5.
Quinolone antibiotics are a crucial class of synthetic antibacterial agents, widely utilized due to their broad spectrum of antibacterial activity. Due to the development of antimicrobial resistance, the potency of quinolone drugs decreased. Many conventional methods have been developed to elevate amination rate and to improve yield. These methods are generally characterized by prolonged reaction durations, high boiling solvents, harsh conditions, costly reagents and excessive heat generation, which have adversely affected the therapeutic efficacy of these compounds. Recently, green chemistry has focused on sustainable chemistry-dependent quinolone analogue synthesis methods that significantly reduce bacterial infections. These methods include one-pot synthesis, photoredox catalysis, phase transfer catalysis, ultrasonic irradiation, microwave-assisted, green solvent and catalyst-free synthesis, which often utilize energy-efficient, non-toxic and less time-consuming techniques, aligning with green chemistry principles to improve safety and environmental impact. Researchers continuously explore innovative approaches to applying these methods in synthetic reactions. This review includes a comprehensive analysis of synthetic literature from the past 15 years from Scopus, PubMed, Embase and WOS using keywords, such as green chemistry, quinolone and antibacterial, highlighting significant advancements and emerging trends. This work's importance lies in its extensive literature overview on green synthesis methods for quinolones and related heterocyclic compounds. Furthermore, to provide useful information for the generation of future antibacterial drugs, some structural-activity relationship studies and in silico studies have also been included to investigate the stable binding interactions between quinolone leads and various target proteins.
喹诺酮类抗生素是一类至关重要的合成抗菌剂，因其广泛的抗菌活性而被广泛使用。由于抗菌耐药性的发展，喹诺酮类药物的效力有所下降。人们已经开发出许多传统方法来提高胺化率和产率。这些方法的特点通常是反应时间长、使用高沸点溶剂、条件苛刻、试剂成本高以及产生过多热量，这些都对这些化合物的治疗效果产生了不利影响。最近，绿色化学专注于依赖可持续化学的喹诺酮类似物合成方法，这些方法能显著减少细菌感染。这些方法包括一锅合成、光氧化还原催化、相转移催化、超声辐射、微波辅助、绿色溶剂和无催化剂合成，它们通常采用节能、无毒且耗时较少的技术，符合绿色化学原则，以提高安全性和环境影响。研究人员不断探索将这些方法应用于合成反应的创新途径。本综述使用“绿色化学”“喹诺酮”和“抗菌”等关键词，对过去15年来自Scopus、PubMed、Embase和WOS的合成文献进行了全面分析，突出了重大进展和新趋势。这项工作的重要性在于其对喹诺酮及相关杂环化合物绿色合成方法的广泛文献综述。此外，为了为未来抗菌药物的研发提供有用信息，还纳入了一些构效关系研究和计算机模拟研究，以研究喹诺酮先导化合物与各种靶蛋白之间的稳定结合相互作用。
