World Journal of
Pharmaceutical and Life Sciences

AZETIDINE: STRUCTURAL FEATURES, SYNTHETIC APPROACHES, AND THERAPEUTIC POTENTIAL

Mr. Abhishek B. Pawar*, Mr. Vishal S. Kavathekar, Ms. Mrudula P. More

ABSTRACT

Azetidine, a saturated four-membered heterocyclic amine that includes nitrogen, has gained considerable interest due to its distinctive structural characteristics, notable ring strain, and adaptable reactivity profile, establishing it as an important framework in medicinal chemistry, organic synthesis, and materials science. Its small ring structure provides unique physicochemical characteristics, such as increased reactivity and the ability for various functionalization. Which support its extensive therapeutic uses. In recent decades, considerable researchhas concentrated synthesis, structural alteration, and various biological assessment of azetidine derivatives, underscoring their potential pharmacological activities, including antibacterial, antifungal, antiviral, anticancer, anti-inflammatory, antimalarial and antidiabetic properties. A range of synthetic approaches has been established to azetidine structures, encompassing cyclization and cycloaddition reactions, metal-catalyzed methods, multicomponent reactions (MCR), and ring-expansion strategies derived from aziridines and imines. Significantly, methods like [2+2] cycloadditions of imines with carbonyl compounds or ketenes, metal-catalyzed cycloaddition of imines with alkenes, and multicomponent reactions utilizing heterocyclic precursors have enabled the effective and stereoselective production of structurally varied azetidine derivatives. These synthetic development have been essential in facilitating the investigation of structure activity relationship and enhance biological activity. The therapeutic promise of azetidine derivatives is highlighted by their integration into multiple pharmacophores, such as β-lactams, thiazolidinones, and benzazole, which demonstrate strong antimicrobial, anticancer, anti-inflammatory, and antiviral properties. Azetidine-derived compounds have shown effectiveness against several pathogens.

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