Design, synthesis and antimicrobial evaluation of novel benzoxazole derivatives

作者：Zhang, Wei; Liu, Jingbao; Macho, Jocelyn M.; Jiang, Xizhen; Xie, Dongsheng; Jiang, Faqin; Liu, Wenlu^*; Fu, Lei^*

来源：European Journal of Medicinal Chemistry, 2017, 126: 7-14.

DOI：10.1016/j.ejmech.2016.10.010

• Antibacterial activity
• Minimum inhibitory concentration
• Benzoxazole
• Propanoic acid

The synthesis of (S)-2-(4-tert-butylphenoxy)-3-(benzoxazol-5-yl) propanoic acid derivatives (2a-k) were described and their in vitro antibacterial activities were determined against Gram-negative and -positive bacteria. These compounds were found to exert a broad spectrum of activity against the screened bacteria, but poor MIC values were found for Candida albicans fungi. Compound 2b bearing a hydrophobic aromatic tie was the most active derivative against all bacteria studied with MIC values ranging from 0.098 to 0.78 mu g/mL. The activity of 2b against B. subtilis was 2-fold higher than Penicillin, and 8-to 510-fold higher than other control antibiotics.

• 出版日期2017-1-27
• 单位上海交通大学