Synthesis and biological evaluation of 1, 3-diaryl pyrazole derivatives as potential antibacterial and anti-inflammatory agents. Issue 22 (15th November 2015)

• Record Type: Journal Article
• Authors: Li, Ya-Ru; Li, Chao; Liu, Jia-Chun; Guo, Meng; Zhang, Tian-Yi; Sun, Liang-Peng; Zheng, Chang-Ji; Piao, Hu-Ri
• Is Part Of: Bioorganic & medicinal chemistry letters. Volume 25:Issue 22(2015)
• Page Start: 5052
• Page End: 5057
• Publication Date: 2015-11-15
• Subjects: Pyrazole -- Aminoguanidine -- Furan -- Antibacterial activity -- Anti-inflammatory activity; Bioorganic chemistry -- Periodicals; Pharmaceutical chemistry -- Periodicals; 572
• DOI: 10.1016/j.bmcl.2015.10.028
• Languages: English
• ISSNs: 0960-894X

Abstract

Graphical abstract: Abstract: Three series of 1, 3-diaryl pyrazole derivatives bearing aminoguanidine or furan-2-carbohydrazide moieties have been synthesized, characterized and evaluated for antibacterial and anti-inflammatory activities. Most of the synthesized compounds showed potent inhibition of several Gram-positive bacterial strains (including multidrug-resistant clinical isolates) and Gram-negative bacterial strains with minimum inhibitory concentration values in the range of 1–64 μg/mL. Compounds6g, 6l and7l presented the most potent inhibitory activity against Gram-positive bacteria (e.g. Staphylococcus aureus 4220), Gram-negative bacteria (e.g. Escherichia coli 1924) and the fungus, Candida albicans 7535, with minimum inhibitory concentration values of 1 or 2 μg/mL. Compared with previous studies, these compounds exhibited a broad spectrum of inhibitory activity. Furthermore, compound7l showed the greatest anti-inflammatory activity (93.59% inhibition, 30 min after intraperitoneal administration), which was more potent than the reference drugs ibuprofen and indomethacin.