Current Organic Chemistry - Volume 29, Issue 11, 2025

Compounds containing the 1,2,4-triazole substructure have been shown to have broad biological activities. Many drugs with a 1,2,4-triazole structure have been developed and proven: for example, ribavirin (antiviral), fluconazole, itraconazole, voriconazole (antifungal), alprazolam (tranquilizer), estazolam (hypnotic, sedative), anastrozole, vorozole and letrozole (as non-steroidal aromatase inhibitors). Given the importance of 1,2,4-triazole scaffolds, the synthesis of their derivatives has attracted much attention. This review deals with the synthetic methods of 1,2,4-triazole compounds in the past 20 years and illustrates selected reactions of this class of compounds. Various biological activities of 1,2,4-triazoles as antifungal, antibacterial, anticancer, anticonvulsant, antituberculosis, antiviral, antiparasitic, analgesic, anti-inflammatory, and anthelmintic agents are also discussed.

The crucial need for sustainable and ecologically benign synthetic methodologies has propelled the exploration of catalytic systems that symbolize green chemistry principles. Zirconia, known for its exceptional catalytic properties and environmental compatibility, emerges as a promising catalyst for the synthesis of heterocyclic compounds. Parallelly, the one-pot multicomponent approach enhances the efficiency of the synthetic process, offering advantages such as reduced reaction steps, atom economy, and overall resource optimization. The Eco-friendly nature of zirconia catalysts, coupled with the versatility of one-pot multicomponent reactions, not only streamlines synthetic procedures but also addresses the pressing demand for sustainable protocols in contemporary organic synthesis. This comprehensive review systematically explores the current progress in zirconia-catalyzed one-pot multicomponent reactions to get various heterocycles and discusses the key advancements, reaction mechanisms, and the impact of reaction conditions on the catalytic efficiency of zirconia. Insights from this review will lead a path to the development of innovative and environmentally conscious strategies for the generation of diverse heterocycles, catering to the evolving landscape of green chemistry and green practices in the domain of organic synthesis.

Imidazoline is often a heterogeneous 5-membered ring structure with two nitrogen atoms. The heterocyclic compounds with an imidazoline moiety are a promising scaffold for investigating medicinal potential. The imidazoline nucleus with an oxo group at the 5^th, 2^nd, or 4^th position exhibits a wide spectrum of antibacterial and antifungal activity, as well as antiviral, anti-inflammatory, anticancer, analgesic, antihypertensive, antioxidant, and enzyme-inhibiting properties. Oxo-imidazoline derivatives are a fascinating class of chemicals that have attracted a lot of research recently because of their numerous biological actions. The primary objective of this paper is to review the synthesis and diverse biological activity of oxo-imidazoline derivatives literature from previous years. The synthesis of oxo-imidazoline derivatives is a prominent topic of study in organic chemistry because of their wide range of biological activity and possible medical uses. This review provides an extensive overview of synthetic pathways employed to prepare oxo-imidazoline derivatives with excellent biological activities. Oxo-imidazoline derivatives are synthesized using a variety of techniques, including oxidative cyclization, amino acid cyclization, base-catalyzed, diamine ring closure metal-catalyzed cyclizations, and so on are discussed in this review. This review also emphasizes the importance of synthetic methodology development in enabling efficient access to oxo-imidazoline derivatives and their analogs, allowing for further investigation of their biological and pharmacological properties. This review also aims to provide a comprehensive overview of the various biological properties such as anti-microbial (anti-fungal & anti-bacterial), anti-cancer, antioxidant, anti-inflammatory, analgesics, anti-virus, and miscellaneous activities exhibited by potent oxo imidazoline derivatives. More than 50 scientific articles presenting more than 80 compounds have been reviewed. Figures and tables provide the most pertinent data that have been carefully extracted and organized.

N-acyl tetrahydrothienopyridine derivatives serve as important structural motifs in bioorganic chemistry. Restricted rotation of C-N bond in such molecules gives rise to two distinct chemical environments. Thienopyridine derivatives 4a-4i were synthesized and characterised by ¹H and ¹³C NMR spectroscopy. The NMR spectra reveal a doubling of signals, which suggests the presence of two rotamers in the solution. Variable temperature (VT) ¹H-NMR studies supported this hypothesis. The NOESY analysis confirmed that Z-rotamer is present in major form as compared to E-rotamer. The results were further corroborated through density functional theoretic calculations.