Synthesis and antibacterial activities of novel sulfonamide derivatives containing a fused-ring
10.16438/j.0513-4870.2020-1810
- VernacularTitle:稠环磺酰胺衍生物的合成与抗菌活性研究
- Author:
Jia-qiang YANG
;
Yue WANG
;
Xu-rong ZHOU
;
Xue-jiao WU
- Publication Type:Research Article
- Keywords:
sulfanilamide;
fused-ring compound;
phosphonate;
synthesis;
antibacterial activity
- From:
Acta Pharmaceutica Sinica
2021;56(3):835-840
- CountryChina
- Language:Chinese
-
Abstract:
To find antibacterial candidate compounds, eighteen novel sulfonamide derivatives containing a fused-ring were designed and synthesized on the basis of previous studies, with structures confirmed by 1H NMR, 13C NMR and MS. Antibacterial activities of the products were evaluated by the agar dilution method. The results show that these derivatives have different degrees of inhibitory activity on the tested bacteria, with the compounds IIi and IIr the most potent. The MIC of IIi for S. aureus, E. coli and MRSA was 8, 32 and 16 μg·mL-1, respectively, and the MIC of the IIr was 8, 64 and 32 μg·mL-1, respectively. The anti-MRSA activities of the two compounds is significant and is worthy of further structural optimization and study.
