Design, synthesis and biological evaluation of 8-hydroxyquinoline derivatives as potential clostridium difficile antibiotics
10.12206/j.issn.2097-2024.202303021
- VernacularTitle:8-羟基喹啉衍生物作为潜在的艰难梭菌抗生素的设计、合成和活性评价
- Author:
Tengfei YE
1
;
Tao CHENG
1
;
Ping SONG
1
;
Weili JI
1
;
Xiaolan BIAN
1
Author Information
1. Department of Pharmacy, Luwan Branch of Ruijin Hospital, School of Medicine, Shanghai Jiaotong University, Shanghai 200020, China.
- Keywords:
clostridium difficile;
anti-infection;
8-hydroxyquinoline derivatives;
structure-activity relationship
- From:
Journal of Pharmaceutical Practice
2023;41(12):737-740
- CountryChina
- Language:Chinese
-
Abstract:
Objective To find a more effective alternative therapy for antibiotic therapy and fecal microbiota transplantation in current primary treatment of clostridioides difficile infection (CDI) because of the high recurrence rate. Methods A series of 8-hydroxyquinoline derivatives were designed and synthesized based on 8-hydroxyquinoline scarffold. Results The activity test against C. difficile showed that most of the molecules exhibited good antibacterial activity against C. difficile, and compound 6f showed attractive anti-C. difficile activity. Conclusion A new type of 8-hydroxyquinoline derivatives with anti-clostridium difficile was found, which could be used as good lead compounds for further development.
