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Microwave-Assisted Preparation of 1-Aryl-1H-pyrazole-5-amines
Published on: June 23, 2019
Synthesis and antimicrobial activity evaluation of pyrazole derivatives containing imidazothiadiazole moiety
Lan-Ying Han1, Jing-Xin Sun1, Chuang Liu1
1Key Laboratory of Natural Medicines of the Changbai Mountain, Ministry of Education, College of Pharmacy, Yanbian University, Yanji, China.
Aim:
The purpose of this work was to investigate the antimicrobial activity of pyrazole derivatives (21a - i and 23a - o) synthesized.
Materials & Methods:
The pyrazole derivatives were synthesized, molecular docked and tested for their antimicrobial activity, cytotoxicity, and hemolysis rate.
Results:
Most of the target compounds showed high selective inhibitory activity against multi-drug resistance compared with other strains. Of these, compounds 21c (MIC = 0.25 µg/mL) and 23 h (MIC = 0.25 µg/mL) showed the strongest antibacterial activity, which was 4-flods than that of the positive control compound gatifloxacin (MIC = 1 µg/mL). Furthermore, compound 23 h showed no cytotoxicity to human LO2 cells, and did not show hemolysis even at ultra-high concentration.
Conclusion:
These results prompted that these compounds are valuable for further development as antimicrobial agents.
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