Synthesis and antibacterial activity of D-glucosamine-fluoroquinolone derivatives
10.16438/j.0513-4870.2023-0227
- VernacularTitle:D-氨基葡萄糖氟喹诺酮衍生物的合成及其抗菌活性研究
- Author:
Wen-wen XIE
1
;
Li FAN
1
;
Jun-hua HU
2
;
Yu-lu SONG
1
;
Tian-fu TAN
1
;
Jia LI
1
;
Na CHEN
2
;
Da-cheng YANG
1
Author Information
1. Key Laboratory of Applied Chemistry of Chongqing Municipality, School of Chemistry and Chemical Engineering, Southwest University, Chongqing 400715, China
2. Citrus Research Institute, Southwest University, Chongqing 400712, China
- Publication Type:Research Article
- Keywords:
italic>D-glucosamine;
fluoroquinolone;
anti-human pathogen activity;
activity against citrus ulcer bacteria
- From:
Acta Pharmaceutica Sinica
2023;58(11):3389-3399
- CountryChina
- Language:Chinese
-
Abstract:
Based on the idea of modification of sugar drugs, or transforming other active substances with sugar molecules, sixteen D-glucosamine-fluoroquinolone (FQ) derivatives were designed by combining D-glucosamine with FQs and synthesized by a multi-step reaction with shared intermediates. The assay results of anti-human pathogenic bacteria and anti-citrus canker showed that the inhibitory activities of two target molecules TM2b and TM2d against Staphylococcus aureus ATCC14125 were stronger than those of all tested positive control drugs, and the inhibitory rates of target molecules TM2m and TM2n against citrus canker were higher than that of the positive control streptomycin at the concentrations of 0.5 and 0.2 µg·mL-1, respectively, which all were worthy of further study. In this study, a series of novel molecules composed of D-glucosamine and FQs were synthesized for the first time, and super antibacterial molecules were found, which expanded the types and biological activities of D-glucosamine derivatives.
