Synthesis of carbohydrate-substituted isoxazoles and evaluation of their antitubercular activity

[摘要] Eight new sugar-substituted isoxazoles were synthesized by a 1,3-dipolar cycloaddition reaction of aromatic nitrile oxides with carbohydrate-substituted alkynes. Products were screened for antimycobacterial activity against the Mycobacterium tuberculosis H37Rv strain. Four compounds, 5e–h , significantly inhibit growth of the bacterial strain with a minimum inhibitory concentration (MIC) of 3.125 μg/mL.

[学科分类] 内科医学

[关键词] aromatic nitrile oxides;1;3-dipolar cycloaddition;isoxazole;Mycobacterium tuberculosis;propargyl O-glycoside