Discovery of 4-nitro-3-phenylisoxazole derivatives as potent antibacterial agents derived from the studies of [3 + 2]
Yan Zhang1, Zhiwu Long1, Longjia Yan1,2
1School of Pharmaceutical Sciences, Guizhou University Guiyang 550025 China yile2021@163.com.
Abstract:
Polysubstituted phenylisoxazoles were designed and synthesized to discover new antibacterial agents via [3 + 2] cycloaddition. Thirty-five compounds with a phenylisoxazole scaffold were characterized by NMR, HRMS, and X-ray techniques. After being evaluated against Xanthomonas oryzae (Xoo), Pseudomonas syringae (Psa), and Xanthomonas axonopodis (Xac), 4-nitro-3-phenylisoxazole derivatives were found to better antibacterial activities. Further studies have shown that the EC50 values of these compounds were much better than that of the positive control, bismerthiazol.
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