Medicinal Chemistry - Volume 21, Issue 8, 2025

The 2-isoxazoline scaffold has emerged as a key structure in medicinal chemistry, with great therapeutic potential for a wide range of biological targets. This review investigates the medicinal value of the 2-isoxazoline scaffold, emphasizing its adaptability and usefulness in the development of new medications. Isoxazoline has a wide range of biological actions, including antibacterial, anti-inflammatory, anticancer, and anti-parasitic effects, which are due to their distinct structural features and capacity to interact with a variety of biological processes. The synthesis, functionalization, and pharmacological uses of isoxazoline derivatives are rigorously studied, yielding information about their modes of action and therapeutic value. This review emphasizes the promise of isoxazoline-based molecules in tackling current medical difficulties and lays the way for future research in this vibrant field of medicinal chemistry.

The emergence of multidrug-resistant microbial strains poses a significant challenge to global public health. In response, researchers have been exploring innovative antimicrobial agents with enhanced efficacy and novel mechanisms of action. One promising approach involves the synthesis of hybrid molecules combining azetidinone and azole moieties, capitalizing on the respective antimicrobial properties of both structural elements. Natural and synthetic azetidinone derivatives hold a prominent position among medicinally significant compounds due to their varied and potent antibiotic activities. Interest persists in discovering new synthetic methods and refining existing ones, as well as applying these methods to create novel, biologically active azetidinone derivatives. Additionally, azoles are highly regarded in pharmaceuticals for their broad efficacy, tolerability, and oral availability. By merging these two pharmacophores, researchers aim to create compounds with synergistic or additive antimicrobial effects, potentially overcoming existing resistance mechanisms. Various synthetic strategies, including click chemistry and multicomponent reactions, have been employed to prepare these hybrid molecules efficiently. The antimicrobial potential of azetidinone-azole conjugates has been extensively evaluated against a spectrum of pathogens, including bacteria, fungi, and protozoa. These studies have demonstrated promising results, with several compounds exhibiting potent activity against both Gram-positive and Gram-negative bacteria, as well as clinically relevant fungal strains. Furthermore, SAR studies have provided valuable insights into the key structural features governing the antimicrobial properties of these conjugates, facilitating further optimization and rational design. In conclusion, the development of azetidinone-azole hybrids represents a promising avenue in the quest for novel antimicrobial agents. This study presents a comprehensive overview of recent advancements in synthesis and antimicrobial evaluation of azetidinone-azole conjugates.

The imidazole scaffold is a cornerstone in medicinal chemistry, widely recognized for its extensive range of biological activities and ability to form stable metal complexes. This review article provides a detailed overview of recent advancements in synthesizing, characterization, and biological evaluation of metal-complexed imidazole derivatives. We explored various synthetic strategies to create diverse metal-based imidazole complexes, emphasizing innovations that enhance efficiency and yield. Furthermore, we delve into the biological profiling of imidazole derivatives, summarizing key findings from studies investigating their antimicrobial, antifungal, anticancer, and other therapeutic properties. Special attention is given to metal coordination's role in modulating these compounds' biological activity. The review discusses the synthesis of imidazole-metal complexes, illustrating how metal ions such as copper, zinc, and iron enhance the pharmacological profiles of imidazole derivatives. Thus, the data from numerous studies was collated and analyzed to comprehensively understand the current landscape and future prospects in imidazole chemistry associated with metals. It is a valuable resource for researchers, guiding future investigations and fostering the development of novel metal-based imidazole therapeutics.

Indazole, a heterocyclic molecule, has emerged as a useful scaffold in synthetic and medicinal chemistry due to its broad biological activity and ease of synthesis. This article thoroughly analyzes unique synthetic methods used to diversify indazole derivatives, such as metal-catalyzed reactions, ecologically friendly approaches, and novel multicomponent reactions. These advances have increased the efficiency and selectivity of indazole synthesis and its structural variety, paving the path for new biological applications. Furthermore, indazole-based compounds have demonstrated promising biological activities, particularly as anticancer, antibacterial, and anti-inflammatory medicines. This review summarizes the present state of indazole research, focusing on synthetic techniques and biological features that make indazole an attractive target for future drug discovery.

Pyridazinone, a six-membered heterocyclic molecule, has emerged as an important pharmacophore in drug discovery due to its diverse range of biological actions. This adaptable scaffold has shown tremendous promise in the development of therapeutic medicines for a variety of pharmacological conditions, including anti-inflammatory, anti-cancer, anti-microbial, cardiovascular, and central nervous system illnesses. Pyridazinone derivatives are useful in medicinal chemistry due to their propensity to interact with a wide range of biological targets. This review offers a comprehensive overview of Pyridazinone-based compounds, focusing on their chemical structure, mechanism of action, structure-activity relationship (SAR), and therapeutic uses. Current trends in Pyridazinone research and its potential as a lead chemical for new medication development are also reviewed. Pyridazinone broad range of activity and adaptability highlight its importance in developing pharmacotherapy.

Azaaurones are formed by the replacement of intra-cyclic oxygen of the central core of a five-membered furan ring or any other carbon of aurones by a nitrogen atom. However, 1-azaaurone obtained by the replacement of intra-cyclic oxygen is the most prominent and desirable. They are the bioactive compounds acting as potential anti-inflammatory, anticancer, antibacterial, and antiviral agents. They comprise relatively less explored, pharmacologically active compounds exhibiting diverse biological activities that can act as potential lead compounds in the context of drug development. This review represents a comprehensive and updated overview of the synthetic protocols and biological activities of 1-azaaurones and their derivatives, enabling the readers to know about the vast medicinal potential of azaaurones and their derivatives in different areas and prompt the medicinal chemists to emphasize their further exploration. Furthermore, this review also covers some important Structure-Activity Relationships (SAR), highlighting the most potential compounds in each series, providing pivotal scope for further improvisation.