title: Synthesis and biological evaluation of 5-aryloxypyrazole derivatives bearing a rhodanine-3-aromatic acid as potential antimicrobial agents.
abstract: Three novel series of 5-aryloxypyrazole derivatives have been synthesized and tested for their antibacterial activity. The majority of the synthesized compounds showed potent inhibitory activity against Gram-positive bacteria Staphylococcus aureus 4220, especially against the strains of multidrug-resistant clinical isolates (MRSA3167/3506 and QRSA3505/3519). Among which compounds IIIb, IIIg and IIIm showed the most potent levels of activity (MIC=1 μg/mL) against the multidrug-resistant strains. And cytotoxic activity assay showed that the compounds tested did not affect cell viability on the Human cervical (HeLa) cells at their MICs. The current study therefore suggests that 5-aryloxypyrazoles bearing a rhodanine-3-aromatic acid moiety are promising scaffolds for the development of novel Gram-positive antibacterial agents.
authors.affiliation: Key Laboratory of Natural Resources and Functional Molecules of the Changbai Mountain, Affiliated Ministry of Education, Yanbian University College of Pharmacy, Yanji 133002, PR China.
authors.forename: Chang-Ji
authors.initials: CJ
authors.lastname: Zheng
authors.forename: Ming-Xia
authors.initials: MX
authors.lastname: Song
authors.forename: Liang-Peng
authors.initials: LP
authors.lastname: Sun
authors.forename: Yan
authors.initials: Y
authors.lastname: Wu
authors.forename: Lan
authors.initials: L
authors.lastname: Hong
authors.forename: Hu-Ri
authors.initials: HR
authors.lastname: Piao
mesh_terms: D000447:Aldehydes / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity; D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D002470:Cell Survival / Q000187:drug effects; D024881:Drug Resistance, Bacterial; D004926:Escherichia coli / Q000187:drug effects; D006367:HeLa Cells; D006801:Humans; D008826:Microbial Sensitivity Tests; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000737:chemistry* / Q000633:toxicity; D012236:Rhodanine / Q000737:chemistry*; D013211:Staphylococcus aureus / Q000187:drug effects; D013329:Structure-Activity Relationship
chemical_list: C579643:5-chloro-3-methyl-1-phenyl-1H-pyrazole-4-carbaldehyde; D000447:Aldehydes; D000900:Anti-Bacterial Agents; D011720:Pyrazoles; C031280:pyrazole; D012236:Rhodanine