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Synthesis and Antimicrobial Activity Evaluation of Pyridine Derivatives Containing ImidazoThiadiazole Moiety

Four series of novel pyridine derivatives (17 a–i, 18 a–i, 19 a–e, and 20 a–e) were synthesized and their antimicrobial activities were evaluated. Of all the target compounds, almost half target compounds showed moderate or high antibacterial activity. The 4‐F substituted compound 17 d (MIC=0.5 μg/m...

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Bibliographic Details
Published in:Chemistry & biodiversity 2024-04, Vol.21 (4)
Main Authors: Liu, Yang, Yu‐Xin Jiao, Yan‐Hua Quan, Ming‐Yu Li, Xin‐Yi Huang, Jun‐Zheng Jin, Li, Siqi, Ji‐Shan Quan, Cheng‐Hua Jin
Format: Article
Language:English
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Summary:Four series of novel pyridine derivatives (17 a–i, 18 a–i, 19 a–e, and 20 a–e) were synthesized and their antimicrobial activities were evaluated. Of all the target compounds, almost half target compounds showed moderate or high antibacterial activity. The 4‐F substituted compound 17 d (MIC=0.5 μg/mL) showed the highest antibacterial activity, its activity was twice the positive control compound gatifloxacin (MIC=1.0 μg/mL). For fungus ATCC 9763, the activities of compounds 17 a and 17 d are equivalent to the positive control compound fluconazole (MIC=8 μg/mL). Furthermore, compounds 17 a and 17 d showed little cytotoxicity to human LO2 cells, and did not show hemolysis even at ultra‐high concentration (200 μM). The results indicate that these compounds are valuable for further development as antibacterial and antifungal agents.
ISSN:1612-1872
1612-1880
DOI:10.1002/cbdv.202400135