Regioselective approach to 5-arylsulfonylisoxazoles and their antimicrobial activity

• Artem S. Sazonov,
• Dmitry A. Vasilenko,
• Denis V. Porfiriev,
• Yuri K. Grishin,
• Rimma A. Gazzaeva,
• Alisa P. Chernyshova,
• Maxim A. Kryakvin,
• Anna A. Baranova,
• Vera A. Alferova and
• Elena B. Averina

Beilstein J. Org. Chem. 2026, 22, 592–602, doi:10.3762/bjoc.22.45

• as promising antimicrobial agents and provide new insights into their mechanism of action. Keywords: antimicrobial activity; aromatic nucleophilic substitution; isoxazoles; oxidation; sulfonylisoxazoles; Introduction The isoxazole ring represents an important building block for the synthesis of

• -inflammatory, for the treatment of Alzheimer diseases, etc. [10][11][12][13][14][15][16]. Among the sulfonyl-containing heterocycles with confirmed efficacy against microorganisms (bacteria and fungi), sulfonylisoxazoles have attracted considerable attention as potential antibacterial drugs, with the isoxazole

• core in these compounds being essential for the activity [10]. Representative examples of biological active sulfonylisoxazoles, including marked drugs (see, for example, edonentan, sulfamethoxazole and sulfisoxazole) and compounds with the most promising activity are shown in Figure 1. Also, modern