Azetidines of pharmacological interest

Abstract

Azetidines are almost unexplored among nitrogen‐containing saturated heterocycles due to difficulties associated with their synthesis. However, over the past few years, attempts have been made by scientists to advance their synthetic feasibility. Compounds with the azetidine moiety display an important and diverse range of pharmacological activities, such as anticancer, antibacterial, antimicrobial, antischizophrenic, antimalarial, antiobesity, anti‐inflammatory, antidiabetic, antiviral, antioxidant, analgesic, and dopamine antagonist activities, and are also useful for the treatment of central nervous system disorders and so forth. Owing to its satisfactory stability, molecular rigidity, and chemical and biological properties, azetidine has emerged as a valuable scaffold and it has drawn the attention of medicinal researchers. The present review sheds light on the traditional method of synthesis of azetidine and advancements in synthetic methodology over the past few years, along with its application with various examples, and its biological significance.

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“…The history of the azetidine compounds back to 1907, the Schiff base reaction [2] from aniline and aldehyde Cycloaddition reaction. Chemistry of this has a wide spectrum and essential part in organosynthetic chemistry [3] since the revelation of Alexander Fleming for prepared Penicillin and the need of more active compounds against the activity of bacteria and fungi due to the resistance of the micro-species [4,5]. The molecular action of the β-lactams derivative antibiotic is power selective and irreversible inhabitation when it is use for processing enzymes of developing peptidoglycan layer [6].…”

Monomeric silica supported interaction of TOSMIC with highly functionalized imines: A green approach to azetidines via ABB‐type cycloaddition reaction

“…Azetidines [7] heterocycles are of huge interest as they constitute an imperative class of aza‐hetrocyclics [8]. Azetidines exhibited a broad range of biological activities such as antibacterial [9], anticancer [10], dopamine antagonist, [11] and used in the treatment of multiple sclerosis [12].…”

“…Azetidines [7] heterocycles are of huge interest as they constitute an imperative class of aza-hetrocyclics [8].…”

Synthesis and strain-release reactions of 1-azabicyclo[1.1.0]butanes: an update

“…Strained nitrogen-containing heterocycles are important scaffolds for the development of new small-molecule pharmaceuticals. 1 In particular, the use of azetidines in medicinal chemistry has grown over the recent years because of their improved pharmacokinetic properties compared with their cyclic homologs. 2,3 The presence of the azetidine ring in biologically active molecules confers greater bioavailability and metabolic stability than non strained rings and can improve clinical success due to its 3D character.…”