Synthesis and antimicrobial activity evaluation of pyridine derivatives containing imidazo[2,1-b][1,3,4]thiadiazole moiety

Chem Biodivers. 2024 Feb 29:e202400135. doi: 10.1002/cbdv.202400135. Online ahead of print.ABSTRACTFour series of novel pyridine derivatives (17a-i, 18a-i, 19a-e, and 20a-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 17d (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 17a and 17d are equivalent to the positive control compound fluconazole (MIC = 8 µg/mL). Furthermore, compounds 17a and 17d 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.PMID:38425248 | DOI:10.1002/cbdv.202400135
Source: Chemistry and Biodiversity - Category: Biochemistry Authors: Source Type: research