A Simple, Efficient One‐Pot Synthesis of 2‐Isoxazoline Derivatives and their Antimicrobial Activity

Abstract

Synthesis of substituted 2‐isoxazolines derivatives with sulfone functional groups was accomplished by 1,3‐dipolar cycloaddition reaction. The 1,3‐dipolar nitrile oxides generated in situ by reacting α‐formaldoximes with N‐bromosuccinimide in the presence of triethylamine on reaction with activated alkenes in toluene at room temperature afford the corresponding 2‐isoxazolines in high yields. All the 2‐isoxazoline derivatives were assayed for their antibacterial activities against Staphylococcus aureus, Bacillus cereus, Escherichia coli, and Pseudomonas aeruginosa and antifungal activities against Aspergillus niger and Candida albicans. Most of the compounds showed good antibacterial and antifungal activities.

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“…The isooxazoline is of valuable interest in several fields as biology. Indeed, 2-isoxazolines compounds possess biological activity [8], such as with antifungal [9], antiviral [10], antitumor [11], anticancer [12], Anti-HIV-RT [13], Organics 2021, 2 2 anti-inflammatory [14] and antimicrobial properties [15,16]. The introduction of halogen atoms into isoxazolines has an effect on its physical and chemical properties, allowing interesting and useful properties to appear in various pharmaceutical fields.…”

Synthesis, Antimicrobial and Antioxidant Activities of 2-Isoxazoline Derivatives

“…Isoxazolines are an important class of nitrogen- and oxygen-containing heterocycles that belong to the azoles family, and have gained great importance in the field of medicinal chemistry as anticancer agents [ 1 , 2 , 3 , 4 , 5 , 6 , 7 , 8 ]. They are also reported to possess good antimicrobial, analgesic, anti-inflammatory activities [ 4 ].…”

“…Isoxazoline derivatives exhibit biological and pharmaceutical activities. They also have wide industrial and analytical applications [ 1 , 2 , 3 , 4 , 5 , 6 , 7 , 8 , 13 ]. These observations prompted us to study the synthesis of certain compounds that possess the isoxazoline moiety to study the antibacterial and antioxidant activities of these compounds on different bacterial strains.…”