Microwave-assisted synthesis and antimicrobial activity of 5-trihalomethyl-3-arylisoxazoles

A series of twelve 5-trihalomethyl-3-arylisoxazoles was synthesized and screened for antibacterial and antifungal activities. The compounds were synthesized from the cyclondensation of 1,1,1-trihalo-4-alkoxy-3-alken-2-ones CX ₃C(O)C(R ²)=C(R ¹)OR, where X = Cl and F; R=Me; R ²=H; R ¹=H, Me, F, Cl, Br, and NO₂] with hydroxylamine hydrochloride through a rapid one-pot reaction via microwave irradiation. Some of the 5-trihalomethyl-3-arylisoxazoles exhibited good in vitro anti-Cryptococcus activity. Correspondence: Marcos A. P. Martins, Núcleo de Química de Heterociclos (NUQUIMHE), Centro de Ciências Naturais e Exatas, Departamento de Química, Universidade Federal de Santa Maria, 97.105-900 Santa Maria, RS, Brazil.