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

摘要

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.