Synthesis and antibacterial activities of phosphonate derivatives containing aminothiazoloxime fragment
10.16438/j.0513-4870.2023-0790
- VernacularTitle:含氨基噻唑肟结构的膦酸酯衍生物的合成与抗菌活性研究
- Author:
Yang-mi CHEN
;
Yan AN
;
Xiang-tao DONG
;
Zi-cong LU
;
Jia-qiang YANG
- Publication Type:Research Article
- Keywords:
aminothiazole oxime;
phosphonate;
molecular hybridization;
synthesis;
antibacterial activity
- From:
Acta Pharmaceutica Sinica
2024;59(1):161-165
- CountryChina
- Language:Chinese
-
Abstract:
Based on the principle of molecular hybridization, fifteen compounds were designed and synthesized through the combination of aminothiazoloxime and phosphonate fragment. The results showed that these compounds had better inhibitory effects on the tested bacteria. In particular, the activities of compounds Ⅲf and Ⅲi against S. aureus, E. coli, methicillin-resistant S. aureus (MRSA) and fluoroquinolone-resistant E. coli (FREC) were the most significant, the minimal inhibitory concentration (MIC) of Ⅲf was 1, 8, 4, 16 μg·mL-1 respectively, and the MIC of Ⅲi was 4, 4, 16, 8 μg·mL-1 respectively, which were slightly lower than that of the control drug oxacillin, and their anti-E. coli, MRSA and FREC activities were superior to that of the control drug oxacillin. Their activities to S. aureus were close to that of oxacillin, and to E. coli, MRSA and FREC were superior to that of oxacillin, which is worthy of further study.
