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

“…This is presumably to avoid the competing oxidative side reactions, if the nitrile oxide was generated oxidatively from the aldoxime. In this aim, a suitable dipole is represented by the nitrile oxide, which has been reacted with vinyl derivatives of sulfides, sulfoxides, and sulfones (2)(3)(4)(5)(6) that are prepared according the previous report [15,16]. All the titled compounds have been performed in a single step onepot synthesis (Scheme 1).…”

“…All the titled compounds have been performed in a single step onepot synthesis (Scheme 1). The nitrile oxide 1a-d, derived in situ from araldehyde bromoxime by treatment with triethylamine, was added to the desired vinyl sulfide (2)(3)(4)(5)(6) for the formation of 2-isoxazolines derivatives (7 a-d to 11 a-d ) and showed higher yields. The higher conversions of 2-isoxazoline derivatives are observed without the formation of any by-products even though at 20-to 35-h reaction time ( Table 1).…”

“…They are versatile scaffolds for the synthesis of a wide variety of complex natural products [2] and important pharmacophore in therapeutic chemistry [3,4]. 2-Isoxazolines are also known to exhibit interesting biological activities such as antifungal [5], antibacterial [6], anti-convulsant [7], anti-inflammatory [8], antiviral [9], analgesic [10], and anti-HIV activities [11]. One of the most general methods used to prepare 2-isoxazolines involves 1,3-dipolar cycloaddition between nitrile oxides and olefins [12].…”

Synthesis, Characterization and Antibacterial Evaluation of Some Azole Derivatives

“…[12][13] Isoxazole ring system occupies prime position in the design and synthesis of novel therapeutic agents. In addition to this, they are known to possess antiepileptic, 14 anticancer, 15 antimicrobial, [16][17] immunomodulatory, 18 antinociceptive, 19 anti-inflammatory, 20 antiplatelet, 21 antiulcer 22 activities and even more. During the last decade, most bacterial pathogens have exhibited antimicrobial resistance, and considerable effort has been directed at developing new agents to replace those whose usefulness has been eroded by resistance.…”